Dovitinib lactate hydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dovitinib (TKI258) Lactate 是 Dovitinib 的乳酸盐，Dovitinib 是一种多靶点 RTK 抑制剂，主要针对 III 类 (FLT3/c-Kit)，IC50 为 1 nM/2 nM。

Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

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 (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.

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GPCR/G Protein

Antibacterial

c-Kit| FGFR1| FGFR3| FLT3| VEGFR3/FLT4

Cancer

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915769-50-5

482.51

C24H27FN6O4

>98% (HPLC)

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CC(C(=O)O)O.CN1CCN(CC1)C2=CC3=C(C=C2)N/C(=C\4/C(=C5C(=NC4=O)C=CC=C5F)N)/N3.O

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(-20℃)

With Ice Pack

≥ 2 years