1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3-IN-12

FLT3-IN-12 

Cat. No.: HY-143895
Handling Instructions

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.

FLT3-IN-12 Chemical Structure

FLT3-IN-12 Chemical Structure

CAS No. : 2499966-67-3

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Description

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)[1].

IC50 & Target

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

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].

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), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL)[1].

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

Molecular Weight

432.44

Formula

C21H23F3N6O

CAS No.
SMILES

O=C1C2=CC=C(NC3=NC=C(C(F)(F)F)C(N[[email protected]@H]4CC[[email protected]@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
References
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FLT3-IN-12
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HY-143895
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