1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3-IN-11

FLT3-IN-11 (compound 30) 是一种有效、选择性和具有口服活性的 FLT3 激酶抑制剂,对野生型 FLT3FLT3-D835YIC50 分别为 7.22 nM 和 4.95 nM。FLT3-IN-11 对 FLT3 的选择性高于 c-KIT (>1000 倍)。FLT3-IN-11 具有出色的抗急性髓性白血病 (AML) 活性 (MV4-11 细胞,IC50 为 3.2 nM)。

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FLT3-IN-11 Chemical Structure

FLT3-IN-11 Chemical Structure

CAS No. : 2499966-50-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM)[1].

IC50 & Target

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)[1]

体外研究
(In Vitro)

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y[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-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%[1].

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

分子量

422.45

Formula

C20H25F3N6O

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
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  • 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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产品名称:
FLT3-IN-11
目录号:
HY-143894
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