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Cat. No.: HY-143895

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FLT3-IN-12

FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC₅₀ of 0.75 nM).

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

CAS No.: 2499966-67-3
Formula: C₂₁H₂₃F₃N₆O
Molecular Weight:432.44

Storage:

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

Data Sheet (271 KB)

FLT3-IN-12 Chemical Structure

CAS No.: 2499966-67-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.16 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835F mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835F mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	0.84 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	1.17 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	1.29 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	1398 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	14.5 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L double mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
BaF3	IC₅₀	3.56 nM Compound: 36	Antiproliferative activity against mouse BaF3 cells expressing FLT3-F691L mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-F691L mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
HeLa	IC₅₀	2067.33 nM Compound: 36	Antiproliferative activity against human Hela cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Hela cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
Kasumi 1	IC₅₀	131.1 nM Compound: 36	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
MCF7	IC₅₀	271.3 nM Compound: 36	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
MM1.S	IC₅₀	1208.5 nM Compound: 36	Antiproliferative activity against human MM.1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MM.1S cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 35138851]
MV4-11	IC₅₀	0.75 nM Compound: 36	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 35138851]
MV4-11	IC₅₀	0.75 nM Compound: A1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]
PBMC	IC₅₀	1735.67 nM Compound: 36	Antiproliferative activity against human PBMC cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human PBMC cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
WI-38	IC₅₀	1618.67 nM Compound: 36	Antiproliferative activity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]
Z-138	IC₅₀	>200 nM Compound: 36	Antiproliferative activity against human Z138 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Z138 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 35138851]

In Vitro

FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC₅₀ range is 0.16-14.5 nM^[1].

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

In Vivo

Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W^[1].
FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)_0–∞ of 5278 ng·h/mL), T_1/2 of 3.7 hours, and high maximum plasma concentrations (C_max of 775 ng/mL)^[1].

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

Chemical Information

CAS No. 2499966-67-3
Molecular Weight 432.44
Formula C₂₁H₂₃F₃N₆O
SMILES

O=C1C2=CC=C(NC3=NC=C(C(F)(F)F)C(N[C@@H]4CC[C@@H](CC4)N)=N3)C=C2C=CN1C
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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