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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 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。

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 (K_i, 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Bevacizumab  |  Sunitinib  |  Imatinib  |  Semaxinib  |  SU 5402  |  Heparan Sulfate  |  PD173074  |  5Z-7-Oxozeaenol  |  Cediranib  |  SAR131675  |  AT9283  |  Formotin  |  Gandotinib  |  KW-2449  |  GW806742X  |  Tanshi IIA  |  Lestaurtinib  |  PF-03814735  |  Ferulic acid  |  PD-166866  |  Vatalanib dihydrochloride  |  CP-547632  |  CG-806  |  AST 487  |  Tyrphostin A9  |  Ki20227  |  Motesanib  |  SU14813

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