CAS:1254053-43-4Gilteritinib

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Gilteritinib Cat No. FB02610Cas No. 1254053-43-4

Synonyms: ASP2215

Gilteritinib is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/< 1 nM respectively and shows potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8093 mL
- 9.0463 mL
- 18.0926 mL
- 5 mM
- 0.3619 mL
- 1.8093 mL
- 3.6185 mL
- 10 mM
- 0.1809 mL
- 0.9046 mL
- 1.8093 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

1254053-43-4

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C29H44N8O3

运输

蓝冰

分子量

552.71

别名

ASP2215

溶解度

DMSO	10.0 mg/mL (18.1 mM)
Water	Insoluble
Ethanol	6.0 mg/mL (10.9 mM)

动物实验配方

靶点数据

生物活性

描述Gilteritinib is a FLT3 inhibitor with IC50 value of 0.29 nM for FLT3, and inhibited FLT3, LTK, ALK, and AXL kinases with IC50 values less than 1nM. Gilteritinib exhibited anti-proliferative effect on MV4-11 cells, harboring FLT3-ITD, with IC50 value of 0.92nM post 5 days and accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6 at concentration>1nM post 2h. Also, it inhibited the growth of Ba/F3 cells expressing FLT3-ITD and/or FLT3-D835 mutation with similar activity. Oral administration of Gilteritinib for 28 days achieved complete MV4-11 tumor regression at dose more than 6mg/kg in mice. Further, it decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells.
作用机制Gilteritinib binds to FLT3 at the ATP-binding site.^[2]
动物研究
剂量
Nude Mice: 3 mg/kg^[3] (p.o.), 30 mg/kg^[3] (p.o.)

给药途径
p.o.

动物药代数据
Animal Nude mice^[3]
Dose 3 mg/kg
Administration p.o.
C_max 21.33 ng/ml
T_max 2 h
AUC_{24 h} 156.3 ng·h/ml