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Dovitinib lactate

CAS No. : 692737-80-7

MCE 站：Dovitinib lactate

产品活性：Dovitinib lactate (TKI258 lactate) 是多靶点的酪氨酸激酶抑制剂，抑制 FLT3，c-Kit，FGFR1/3，VEGFR1/2/3 和 PDGFRα/β 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. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2.

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 demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis.

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  |  Formononetin  |  Gandotinib  |  KW-2449  |  GW806742X  |  Tanshinone 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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