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

FLT3-IN-12 是一种有效的、选择性的、具有口服活性的 FLT3 激酶抑制剂,对 FLT3-WTFLT3-D835YIC50 分别为 1.48 nM 和 2.87 nM。FLT3-IN-12 具有比 c-KIT 高的选择性 (>1000 倍)。FLT3-IN-12 具有出色的抗急性髓性白血病活性 (MV4-11细胞,IC50 为 0.75 nM)。

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FLT3-IN-12 Chemical Structure

FLT3-IN-12 Chemical Structure

CAS No. : 2499966-67-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

体外研究
(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.

体内研究
(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.

分子量

432.44

Formula

C21H23F3N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献

FLT3-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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FLT3-IN-12
目录号:
HY-143895
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