FLT3-IN-14

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FLT3-IN-14 is a potent FLT3 inhibitor with IC₅₀s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model.

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FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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Description

IC₅₀ & Target

IC₅₀: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.608 μM Compound: 9c	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
K562	IC₅₀	1.582 μM Compound: 9c	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KCL-22	IC₅₀	0.709 μM Compound: 9c	Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1	IC₅₀	0.265 μM Compound: 9c	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1a	IC₅₀	0.904 μM Compound: 9c	Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	0.014 μM Compound: 9c	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLT-4	IC₅₀	0.591 μM Compound: 9c	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	IC₅₀	0.011 μM Compound: 9c	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
NOMO-1	IC₅₀	1.541 μM Compound: 9c	Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
OCI-AML2	IC₅₀	0.519 μM Compound: 9c	Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
PBL	GI₅₀	> 10 μM Compound: 9c	Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35339838]
PBL	GI₅₀	8.9 μM Compound: 9c	Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 35339838]
THP-1	IC₅₀	1.454 μM Compound: 9c	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]

In Vitro

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC₅₀s of 0.011-1.582 μM^[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI₅₀ greater than 10 μM, in resting lymphocytes^[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner^[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines^[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3^[1].

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

Cell Proliferation Assay

Cell Line:	MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22^[1]
Concentration:	0-10 μM
Incubation Time:	24 hours
Result:	Inhibited the proliferation of these twelve haematological cell lines with IC₅₀s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line:	PBL^[1]
Concentration:	0-10 μM
Incubation Time:	72 hours
Result:	Exhibited low toxicity, with GI₅₀ greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line:	MV4-11^[1]
Concentration:	1, 10 and 50 nM
Incubation Time:	24 and 48 hours
Result:	Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line:	MOLM-13 and MV-14^[1]
Concentration:	25, 50, 75 and 100 nM
Incubation Time:	24 and 48 hours
Result:	Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line:	MV-14^[1]
Concentration:	1, 10 and 50 nM
Incubation Time:	24 hours
Result:	Induced the dephosphorylation of FLT3.

In Vivo

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity^[1].

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

Animal Model:	NOD/SCID female mice (subcutaneously implanted MV4-11)^[1]
Dosage:	1.0 and 3.0 mg/kg
Administration:	IP; daily for 28 days
Result:	Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.

Molecular Weight

472.56

Formula

C₂₅H₂₄N₆O₂S

CAS No.

2620551-45-1

SMILES

CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN4C5=C(SC4=N3)CCC6=CNC=C65)=O)=NO1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022 [Content Brief]

FLT3-IN-14 Related Classifications

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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:

FLT3-IN-142620551-45-1FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaPhosphorylationCell cytotoxicityMOLM-13MV-14NOD/SCID female miceInhibitorinhibitorinhibit

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