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Dovitinib lactate hydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dovitinib lactate hydrate图片
CAS NO:915769-50-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
TKI258 lactate hydrate
CHIR-258 lactate hydrate
产品介绍
Dovitinib lactate hydrate (TKI258 lactate hydrate) 是多靶点的酪氨酸激酶抑制剂,抑制FLT3c-KitFGFR1/3VEGFR1/2/3PDGFRα/βIC50值分别为 1,2,8/9,10/13/8,27/210 nM。
生物活性

Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor withIC50s of 1, 2, 8/9, 10/13/8, 27/210 nM forFLT3,c-Kit,FGFR1/3,VEGFR1/2/3andPDGFRα/β, respectively[1].

IC50& Target[1]

FLT3

1 nM (IC50)

c-Kit

2 nM (IC50)

FGFR1

8 nM (IC50)

FGFR3

9 nM (IC50)

VEGFR1

1 nM (IC50)

VEGFR3

8 nM (IC50)

VEGFR2

13 nM (IC50)

PDGFRα

27 nM (IC50)

PDGFRβ

210 nM (IC50)

体外研究
(In Vitro)

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50values of 25 nM. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively[1].

体内研究
(In Vivo)

Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice[1].

Clinical Trial
分子量

500.52

Formula

C24H29FN6O5

CAS 号

915769-50-5

中文名称

多韦替尼乳酸盐水合物

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.