FLT3/ITD-IN-4

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FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC₅₀ of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.

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

FLT3/ITD-IN-4 Chemical Structure

CAS No. : 2278278-04-7

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

FLT3-ITD

2.3 nM (IC₅₀)

FLT3 D835Y

4.84 nM (IC₅₀)

RET

277 nM (EC₅₀)

FLT3

443 nM (EC₅₀)

ZAK/MLTK

1069 nM (EC₅₀)

CDK16/Cyclin Y

1768 nM (EC₅₀)

DDR2

2494 nM (EC₅₀)

EPHA7

3255 nM (EC₅₀)

NTRK1

3857 nM (EC₅₀)

MAP4K4

5737 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
EJM	IC₅₀	2.152 μM Compound: 16	Cytotoxicity against human EJM cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human EJM cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
EOL1	IC₅₀	< 0.001 μM Compound: 16	Cytotoxicity against human EOL1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human EOL1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
HL-60	IC₅₀	2.985 μM Compound: 16	Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
IM-9	IC₅₀	1.382 μM Compound: 16	Cytotoxicity against human IM-9 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human IM-9 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
KG-1	IC₅₀	0.383 μM Compound: 16	Cytotoxicity against human KG-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human KG-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
KG-1a	IC₅₀	0.403 μM Compound: 16	Cytotoxicity against human KG-1a cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human KG-1a cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
L-363	IC₅₀	0.339 μM Compound: 16	Cytotoxicity against human L-363 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human L-363 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
LP-1	IC₅₀	0.22 μM Compound: 16	Cytotoxicity against human LP-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human LP-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
MOLM-13	IC₅₀	< 0.001 μM Compound: 16	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
MV4-11	IC₅₀	< 0.001 μM Compound: 16	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
MV4-11	IC₅₀	0.64 nM Compound: 16	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by trypan blue dye exclusion method Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by trypan blue dye exclusion method	[PMID: 32199135]
NOMO-1	IC₅₀	1.638 μM Compound: 16	Cytotoxicity against human NOMO-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human NOMO-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
OCI-AML2	IC₅₀	1.192 μM Compound: 16	Cytotoxicity against human OCI-AML2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human OCI-AML2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
OCI-AML-3	IC₅₀	3.424 μM Compound: 16	Cytotoxicity against human OCI-AML-3 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human OCI-AML-3 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
OPM-2	IC₅₀	0.343 μM Compound: 16	Cytotoxicity against human OPM-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human OPM-2 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
RPMI-8226	IC₅₀	1.679 μM Compound: 16	Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
THP-1	IC₅₀	1.686 μM Compound: 16	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]
U-266	IC₅₀	2.163 μM Compound: 16	Cytotoxicity against human U-266 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay Cytotoxicity against human U-266 cells assessed as reduction in cell viability after 4 days by CellTiter-Blue assay	[PMID: 32199135]

Molecular Weight

458.47

Formula

C₂₅H₂₂N₄O₅

CAS No.

2278278-04-7

SMILES

CC(C)(C1=CC(NC(NC2=CC=C3OC(C(C4=CC5=C(N4)C=CC(O)=C5)=O)=CC3=C2)=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]. Sellmer A, et al. A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. Eur J Med Chem. 2020 May 1;193:112232. [Content Brief]

FLT3/ITD-IN-4 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.

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