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Dovitinib

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产品价格:电议      采购度:1597      原产地:美洲

发布时间:2021/7/23 23:35:32      所属地区:上海 上海市

简要描述:

Dovitinib (CHIR-258) 是多靶点的酪氨酸激酶抑制剂,抑制 FLT3,c-Kit,FGFR1/FGFR3,VEGFR1/VEGFR2/VEGFR3 和 PDGFRα/PDGFRβ 的 IC50 值分别为 1,2,8/9,10/13/8,27/210 nM。

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标签:CHIR-258   

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Dovitinib

CAS No. : 405169-16-6

MCE 站:Dovitinib

产品活性:Dovitinib (CHIR-258) 是多靶点的酪氨酸激酶抑制剂,抑制 FLT3c-KitFGFR1/FGFR3VEGFR1/VEGFR2/VEGFR3PDGFRα/PDGFRβIC50 值分别为 1,2,8/9,10/13/8,27/210 nM。

研究领域:Protein Tyrosine Kinase/RTK

作用靶点:FLT3  |  c-Kit  |  FGFR  |  VEGFR  |  PDGFR

In Vitro: Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50?values 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 IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Dovitinib significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells. Dovitinib enhances the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. Dovitinib also stimulates the translocation of phosphorylated Smad1/5/8 into the nucleus and phosphorylation of mitogen-activated protein kinases, including ERK1/2 and p38. Dovitinib strongly inhibits both the interaction of TNIK with ATP (Ki, 13 nM) and the activation of Wnt signaling effectors such as β-catenin and TCF4. Dovitinib also induces caspase-dependent apoptosis in IM-9 cells without significant cytotoxicity in PBMCs.

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. Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg.

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