Nilotinib (Synonyms: AMN107)

Name: Nilotinib
Brand: MedChemExpress
SKU: HY-10159
Rating: 5.0 (46 reviews)

Cat. No.: HY-10159 Purity: 99.94%: Data Sheet
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Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

For research use only. We do not sell to patients.

Nilotinib Chemical Structure

CAS No. : 641571-10-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of Nilotinib:

Nilotinib-d₆ In-stock
Nilotinib-d₃ In-stock
Nilotinib monohydrochloride monohydrate In-stock
Nilotinib hydrochloride dihydrate In-stock
Nilotinib-¹³C,d₃ Get quote
Nilotinib hydrochloride Get quote
Nilotinib (Standard) Get quote

44 Publications Citing Use of MCE Nilotinib

Proliferation Assay

IHC

: Nilotinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]; Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).

: Nilotinib purchased from MedChemExpress. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23. [Abstract]; Cell cycle analysis of HT93A cells by flow cytometry. Cells are treated with 100 nM Nilotinib and 50 ng/mL G-CSF alone or in combination for 48 h before the cell cycle is analyzed. Nilotinib treatment increases the fraction of cells in G0/G1 phase and decreased the S+G2/M-phase fraction.

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Abl Bcr-Abl

Biological Activity
Purity & Documentation
References
Customer Review

Description

Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

IC₅₀ & Target

Bcr-Abl^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.63 μM Compound: 2	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 23521020]
BJ	IC₅₀	12.8 μM Compound: Tasigna	Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay	[PMID: 24835982]
BaF3	GI₅₀	0.004 μM Compound: Nilotinib	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.017 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.021 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.023 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.025 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.0546 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.202 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.47 μM Compound: Nilotinib	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	0.87 μM Compound: Nilotinib	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.093 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.1 μM Compound: Nilotinib	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.3 μM Compound: Nilotinib	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	1.4 μM Compound: Nilotinib	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	2.1 μM Compound: Nilotinib	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	4.1 μM Compound: Nilotinib	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	GI₅₀	> 10 μM Compound: Nilotinib	Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
BaF3	IC₅₀	0.003 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.0095 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.022 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.12 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.12 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.13 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.15 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.16 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	0.17 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	1 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	1.2 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	1.4 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	1.54 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	10 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	10 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	10.3 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	11.8 nM Compound: Nilotinib	Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
BaF3	IC₅₀	120 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	15.1 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	150 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	159 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	16 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	17 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	190 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	2.1 nM Compound: Nilotinib	Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	2.7 μM Compound: Nilotinib	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay	[PMID: 26814890]
BaF3	IC₅₀	2.9 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	21 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	21.1 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	25 nM Compound: Tasigna, AMN107	Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells	[PMID: 20817538]
BaF3	IC₅₀	2800 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	292 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	3 μM Compound: 2	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 23301703]
BaF3	IC₅₀	314 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	38.6 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	4.2 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	40750 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	473 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	49 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	5.1 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	6.34 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	60.7 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	62 nM Compound: Tasigna, AMN107	Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells	[PMID: 20817538]
BaF3	IC₅₀	63 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	65.2 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	67 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	775 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	8.38 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	80 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	87.2 nM Compound: 2, AMN107	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay	[PMID: 23088644]
BaF3	IC₅₀	930 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	95 nM Compound: Nilotinib	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	9500 nM Compound: Nilotinib	Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	> 1 μM Compound: 1	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 26195136]
BaF3	IC₅₀	> 100 nM Compound: Nilotinib	Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay	[PMID: 34011155]
BaF3	IC₅₀	> 10000 nM Compound: Tasigna, AMN107	Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3 Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3	[PMID: 20817538]
BaF3	IC₅₀	> 2000 nM Compound: Chemical probe: AMN107	Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis	[PMID: 15930265]
CHO	IC₅₀	4.7 μM Compound: nilotinib	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
Daoy	IC₅₀	6 μM Compound: Nilotinib	Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by Alamar blue dye based fluorescence spectrophotometric assay Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by Alamar blue dye based fluorescence spectrophotometric assay	[PMID: 33636537]
GIST882	IC₅₀	151 nM Compound: Tasigna, AMN107	Antiproliferative activity against human GIST882 cells Antiproliferative activity against human GIST882 cells	[PMID: 20817538]
H9c2	IC₅₀	21.33 μM Compound: Nilotinib	Cytotoxicity against rat H9c2 cells incubated for 48 hrs and measured by MTT assay Cytotoxicity against rat H9c2 cells incubated for 48 hrs and measured by MTT assay	[PMID: 36283251]
HCT-116	IC₅₀	2.39 μM Compound: 2	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 23521020]
HCT-116	IC₅₀	5.75 μM Compound: Nilotinib	Antiproliferative activity against human HCT-116 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33246255]
HEK293	IC₅₀	0.128 μM Compound: 38	Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate	[PMID: 35944339]
HEK293	IC₅₀	0.147 μM Compound: 38	Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate	[PMID: 35944339]
HEK293	IC₅₀	0.5 μM Compound: nilotinib	Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861) Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)	[PMID: 35163125]
HEK293	IC₅₀	3.7 nM Compound: Tasigna, AMN107	Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA	[PMID: 20817538]
HEK293	IC₅₀	5.2 nM Compound: Tasigna, AMN107	Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA	[PMID: 20817538]
HEK293	IC₅₀	677 nM Compound: Tasigna, AMN107	Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA	[PMID: 20817538]
HEK293	IC₅₀	8.2 μM Compound: Nilotinib	Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38006642]
HEK293	IC₅₀	8.3 μM Compound: AMN107	Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay	[PMID: 35944901]
HEK293	IC₅₀	8.4 μM Compound: Nilotinib	Cytotoxicity against HEK293 cells incubated for 48 hrs and measured by MTT assay Cytotoxicity against HEK293 cells incubated for 48 hrs and measured by MTT assay	[PMID: 36283251]
HEL	GI₅₀	3.9 μM Compound: Nilotinib	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
Jurkat	IC₅₀	> 1000 nM Compound: Nilotinib	Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	GI₅₀	0.002 μM Compound: Nilotinib	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
K562	GI₅₀	26 nM Compound: AMN107	Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	GI₅₀	> 1000 nM Compound: AMN107	Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	IC₅₀	0.0039 μM Compound: Nilotinib	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26814890]
K562	IC₅₀	0.015 μM Compound: 2	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 23521020]
K562	IC₅₀	0.022 μM Compound: 1	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 26195136]
K562	IC₅₀	1.8 nM Compound: Nilotinib	Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34011155]
K562	IC₅₀	1.8 μM Compound: Nilotinib	Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method	[PMID: 28280261]
K562	IC₅₀	2.4 μM Compound: Tasigna	Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay	[PMID: 24835982]
K562	IC₅₀	21 nM Compound: Tasigna, AMN107	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 20817538]
K562	IC₅₀	260 nM Compound: Nilotinib	Antiproliferative activity against human imatinib-resistant K562 cells Antiproliferative activity against human imatinib-resistant K562 cells	[PMID: 21376587]
K562	IC₅₀	28 nM Compound: Nilotinib	Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method	[PMID: 28280261]
K562	IC₅₀	42 nM Compound: Tasigna, AMN107	Inhibition of BCR-ABL1 autophosphorylation in human K562 cells Inhibition of BCR-ABL1 autophosphorylation in human K562 cells	[PMID: 20817538]
K562	IC₅₀	6.5 nM Compound: Nilotinib	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 21376587]
K562	IC₅₀	89.13 μM Compound: Nilotinib	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 23538233]
K562	IC₅₀	< 100 nM Compound: Nilotinib	Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method	[PMID: 28280261]
KBM5	IC₅₀	12 nM Compound: NLT	Cytotoxicity against human KBM5 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human KBM5 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31727471]
KBM5	IC₅₀	2421 nM Compound: NLT	Cytotoxicity against human KBM5 cells expressing IM-resistant Bcr/Abl T315I mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human KBM5 cells expressing IM-resistant Bcr/Abl T315I mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31727471]
L02	IC₅₀	37.03 μM Compound: Nilotinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38006642]
L02	IC₅₀	40.39 μM Compound: Nilotinib	Cytotoxicity against human L02 cells incubated for 48 hrs and measured by MTT assay Cytotoxicity against human L02 cells incubated for 48 hrs and measured by MTT assay	[PMID: 36283251]
MCF7	IC₅₀	6.92 μM Compound: 2	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23521020]
MDA-MB-231	IC₅₀	7.31 μM Compound: Nilotinib	Antiproliferative activity against human MDA-MB-231 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 33246255]
MDA-MB-435S	IC₅₀	2.66 μM Compound: 2	Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay	[PMID: 23521020]
MEG-01	GI₅₀	0.016 μM Compound: Nilotinib	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MOLM-14	GI₅₀	> 10 μM Compound: Nilotinib	Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
MV4-11	GI₅₀	> 10 μM Compound: Nilotinib	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
NCI-H2286	IC₅₀	1.8 μM Compound: Nilotinib	Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay	[PMID: 26191369]
NCI-H23	IC₅₀	3.05 μM Compound: 2	Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H460	IC₅₀	14.41 μM Compound: 2	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 23521020]
NFS-60	IC₅₀	838 nM Compound: Tasigna, AMN107	Antiproliferative activity against mouse M-NFS-60 cells Antiproliferative activity against mouse M-NFS-60 cells	[PMID: 20817538]
SCH	IC₅₀	14.6 μM Compound: 3; AMN107	Antiproliferative activity against human SCH cells assessed as reduction in cell viability Antiproliferative activity against human SCH cells assessed as reduction in cell viability	[PMID: 31923860]
SH-SY5Y	IC₅₀	38.51 μM Compound: Nilotinib	Cytotoxicity against human SH-SY5Y cells incubated for 48 hrs and measured by MTT assay Cytotoxicity against human SH-SY5Y cells incubated for 48 hrs and measured by MTT assay	[PMID: 36283251]
SH-SY5Y	IC₅₀	38.69 μM Compound: Nilotinib	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38006642]
Sf21	IC₅₀	0.158 μM Compound: Nilotinib	Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr in presence of ATP by fluorescence assay Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr in presence of ATP by fluorescence assay	[PMID: 32051094]
T47D	IC₅₀	6.08 μM Compound: 2	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 23521020]
THP-1	IC₅₀	400 nM Compound: Nilotinib	Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as TNF-alpha secretion pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as TNF-alpha secretion pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis	[PMID: 36094045]
U-937	GI₅₀	> 10 μM Compound: Nilotinib	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay	[PMID: 26789553]
U-937	IC₅₀	> 1000 nM Compound: Nilotinib	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]

In Vitro

Nilotinib (AMN107), selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC₅₀<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance^[1].
Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC₅₀ of 4.59±0.97 μM and 11.15±1.48 μM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC₅₀ values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nilotinib (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft^[2].
Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)^[2]
Dosage:	40 mg/kg
Administration:	Oral gavage; daily; 4 weeks
Result:	Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.

Clinical Trial

Molecular Weight

529.52

Formula

C₂₈H₂₂F₃N₇O

CAS No.

641571-10-0

Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=CC(C(F)(F)F)=CC(N2C=NC(C)=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

1 M HCl : ≥ 100 mg/mL (188.85 mM)

DMSO : 12.5 mg/mL (23.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8885 mL	9.4425 mL	18.8850 mL
5 mM	0.3777 mL	1.8885 mL	3.7770 mL
10 mM	0.1889 mL	0.9443 mL	1.8885 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.94 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 4.17 mg/mL (7.88 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20. [Content Brief]

[2]. Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613. [Content Brief]

[3]. Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85. [Content Brief]

[4]. Fujita KI, et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. J Pharm Sci. 2017 Sep;106(9):2632-2641. [Content Brief]

[5]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 1 M HCl	1 mM	1.8885 mL	9.4425 mL	18.8850 mL	47.2126 mL
	5 mM	0.3777 mL	1.8885 mL	3.7770 mL	9.4425 mL
	10 mM	0.1889 mL	0.9443 mL	1.8885 mL	4.7213 mL
	15 mM	0.1259 mL	0.6295 mL	1.2590 mL	3.1475 mL
	20 mM	0.0944 mL	0.4721 mL	0.9443 mL	2.3606 mL
1 M HCl	25 mM	0.0755 mL	0.3777 mL	0.7554 mL	1.8885 mL
	30 mM	0.0630 mL	0.3148 mL	0.6295 mL	1.5738 mL
	40 mM	0.0472 mL	0.2361 mL	0.4721 mL	1.1803 mL
	50 mM	0.0378 mL	0.1889 mL	0.3777 mL	0.9443 mL
	60 mM	0.0315 mL	0.1574 mL	0.3148 mL	0.7869 mL
	80 mM	0.0236 mL	0.1180 mL	0.2361 mL	0.5902 mL
	100 mM	0.0189 mL	0.0944 mL	0.1889 mL	0.4721 mL

Nilotinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nilotinib641571-10-0AMN107AMN 107AMN-107Bcr-AblAutophagytyrosine kinaseantitumorInhibitorinhibitorinhibit

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Nilotinib (Synonyms: AMN107)

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