Brigatinib (Synonyms: AP-26113)

Name: Brigatinib
Brand: MedChemExpress
SKU: HY-12857
Rating: 5.0 (26 reviews)

Cat. No.: HY-12857 Purity: 99.98%: FAQs
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Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC.

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

Brigatinib Chemical Structure

CAS No. : 1197953-54-0

Size	Stock	Quantity
Solution
10 mM * 1 mL in Ethanol	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of Brigatinib:

Brigatinib-¹³C₆ Get quote
Brigatinib-d3 Get quote

26 Publications Citing Use of MCE Brigatinib

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Biological Activity
Protocol
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References
Customer Review

Description

Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC₅₀ of 0.6 nM. Brigatinib can be used for research of NSCLC^[1].

IC₅₀ & Target

IC50: 0.6 nM (ALK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1.359 nM Compound: 6	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
A-431	IC₅₀	709 nM Compound: Brigatinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
A-431	EC₅₀	936 nM Compound: 14	Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	IC₅₀	< 100 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	0.155 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	0.17 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.26 μM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	0.286 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	0.42 μM Compound: Brigatinib	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	0.42 μM Compound: 5	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	0.492 nM Compound: 6	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 35446588]
BaF3	IC₅₀	0.56 μM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.61 μM Compound: 6	Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	1 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	1.91 μM Compound: 6	Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	10 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	12 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	19 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	20 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	EC₅₀	295 nM Compound: 14	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	35 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	36 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	39.9 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	4.191 μM Compound: 9	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	433 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against mouse BaF3 cells harboring del18/T790M/C797S triple mutant assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay	[PMID: 35810715]
BaF3	IC₅₀	47 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	48 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	55.5 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
BaF3	IC₅₀	67.2 nM Compound: 15	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	7.31 μM Compound: Brigatinib	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	8.49 nM Compound: Brigatinib	Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against mouse BaF3 cells overexpressing ALK assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
BaF3	IC₅₀	93 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	98 nM Compound: Brigatinib	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
HEK-293T	IC₅₀	850 nM Compound: Brigatinib	Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs	[PMID: 34138566]
KARPAS-299	GI₅₀	10 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
KARPAS-299	IC₅₀	29 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
LoVo	IC₅₀	2.03 μM Compound: 6	Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay Inhibition of wild type EFGR expressed in human LoVo cell line assessed as inhibition of EGF-stimulated EGFR phosphorylation potency measured after 2 hrs by HRTF assay	[PMID: 34491761]
NCI-H1299	IC₅₀	1.049 μM Compound: 9	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay	[PMID: 35178175]
NCI-H1975	IC₅₀	0.62 μM Compound: Brigatinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	0.64 μM Compound: Brigatinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	1.09 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
NCI-H2228	IC₅₀	31.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell proliferation measured by CCK8 assay	[PMID: 34245852]
NCI-H2228	IC₅₀	58.2 nM Compound: Brigatinib	Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 32179332]
PC-9	IC₅₀	0.829 μM Compound: 9	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	1.11 μM Compound: 9	Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	1.454 nM Compound: 6	Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
PC-9	IC₅₀	599.2 nM Compound: Brigatinib	Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell viability measured after 72 hrs by Celltiter-Glo assay	[PMID: 35413415]
Sf9	IC₅₀	0.001 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k	[PMID: 31718182]
Sf9	IC₅₀	0.001 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki	[PMID: 31718182]
Sf9	IC₅₀	0.13 μM Compound: Brigatinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	[PMID: 31718182]
Sf9	IC₅₀	3 nM Compound: 3	Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	[PMID: 31298540]
SR	IC₅₀	3.3 nM Compound: Brigatinib	Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 34138566]
U-937	IC₅₀	3194 nM Compound: 11q; Brigatinib; AP26113	Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]

In Vitro

Brigatinib potently inhibits the in vitro kinase activity of ALK (IC₅₀, 0.6 nM) and all five mutant variants tested, including G1202R (IC₅₀, 0.6-6.6 nM).
Brigatinib demonstrates a high degree of selectivity, only inhibiting 11 additional native or mutant kinases with IC₅₀ <10 nM. These include ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR (L858R; IC₅₀, 1.5-2.1 nM).
Brigatinib exhibits more modest activity against EGFR with a T790M resistance mutation (L858R/T790M), native EGFR, IGF1R, and INSR (IC₅₀, 29-160 nM) and does not inhibit MET (IC₅₀ >1000 nM).
In cellular assays, brigatinib inhibits ALK and ROS1 with IC₅₀s of 14 and 18 nM, respectively.
Brigatinib inhibits FLT3 and IGF-1R with about 11-fold lower potency (IC₅₀, 148-158 nM) and inhibits mutant variants of FLT3 and EGFR with 15- to 35-fold lower potency (IC₅₀, 211-489 nM).
Brigatinib inhibits cell growth with GI₅₀ values ranging from 503 to 2,387 nM in three ALK-negative ALCL and NSCLC cell lines^[1].
Brigatinib inhibits ALK activity and abrogates proliferation of ALK addicted neuroblastoma cell lines, with IC₅₀ of 75.27 ± 8.89 nM.
Brigatinib inhibits both the ALK-I1171N and the ALK-G1269A mutant receptors at 10 and 4 nM levels, respectively^[3].

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

In Vivo

Brigatinib (10, 25, or 50 mg/kg once daily, p.o.) leads to a dose-dependent inhibition of tumor growth in ALK⁺ Karpas-299 (ALCL) and H2228 (NSCLC) xenograft mouse models. Brigatinib markedly enhances survival of mice bearing ALK⁺ brain tumors compared with PF-02341066^[1].
Brigatinib (10, 25, 50 mg/kg, p.o.) results in dose-dependent antitumor activity, with tumor regressions in a mouse model of NSCLC^[2].

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

Clinical Trial

Molecular Weight

584.09

Formula

C₂₉H₃₉ClN₇O₂P

CAS No.

1197953-54-0

Appearance

Solid

Color

White to light yellow

SMILES

CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1

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:

Ethanol : 10 mg/mL (17.12 mM; Need ultrasonic and warming)

DMSO : 2 mg/mL (3.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7121 mL	8.5603 mL	17.1206 mL
5 mM	0.3424 mL	1.7121 mL	3.4241 mL
10 mM	0.1712 mL	0.8560 mL	1.7121 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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 EtOH stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.86 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.86 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.86 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.

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: 99.98%

Select Batch:

Data Sheet (279 KB) SDS (615 KB)

COA (247 KB) LCMS (107 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief]

[2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief]

[3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Kinase Assay ^[1]	In vitro HotSpot^SM kinase profiling of 289 kinases is performed. The assay is conducted in the presence of 10 μM [³³P]-ATP, using brigatinib concentrations ranging from 0.05 nM to 1 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	Cells are seeded at 15,000 per well with serial dilutions of the indicated inhibitors. After 72 hours cell viability is assessed by resazurin. IC₅₀ values are calculated with GraphPad Prism 6.0 by fitting data to a log (inhibitor concentration) vs. normalized response (variable slope) equation. Each experiment is performed in duplicate and repeated at least three times. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: (1) Eight- to 10-week-old female SCID/beige mice are injected intravenously with 5×10⁶ H3122 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reaches appr 300 mm³ (day zero). Treatments are administered orally for up to 21 consecutive days at a 10 mL/kg dose volume. Subcutaneous tumors are measured two or three times weekly. Tumor volume (in mm³) is calculated using the formula (L×W²)/2. When a tumor reaches 10% of the body weight of the host, the animal is euthanized via CO₂ asphyxiation. (2) Eight- to 10-week old female SCID/beige mice are injected subcutaneously with 2.5×10⁶ Karpas-299 cells per mouse and are randomly selected into treatment groups (n=10) when the average tumor size reached appr 180 mm³ (day zero). Treatments are administered orally for 14 consecutive days at a 10 mL/kg dose volume. Tumor volume is measured and calculated as described for the H3122 model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538 [Content Brief] [2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64. [Content Brief] [3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / Ethanol	1 mM	1.7121 mL	8.5603 mL	17.1206 mL	42.8016 mL
Ethanol	5 mM	0.3424 mL	1.7121 mL	3.4241 mL	8.5603 mL
	10 mM	0.1712 mL	0.8560 mL	1.7121 mL	4.2802 mL
	15 mM	0.1141 mL	0.5707 mL	1.1414 mL	2.8534 mL

Brigatinib 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:

Brigatinib1197953-54-0AP-26113AP26113AP 26113Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246NSCLCcancerALK mutationInhibitorinhibitorinhibit

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Brigatinib (Synonyms: AP-26113)

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