2499966-67-3
2499966-67-3 structure
- Name: FLT3-IN-12
- Chemical Name: FLT3-IN-12
- CAS Number: 2499966-67-3
- Molecular Formula: C21H23F3N6O
- Molecular Weight: 432.44
- Create Date: 2022-05-16 19:01:02
- Modify Date: 2024-01-09 12:20:56
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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].
| Name | FLT3-IN-12 |
|---|
| 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]. |
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| Related Catalog | |
| 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]. |
| 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]. |
| References |
| Molecular Formula | C21H23F3N6O |
|---|---|
| Molecular Weight | 432.44 |