AZM475271

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

AZM475271是Src激酶高效选择性抑制剂，IC50值为5nM，对Flt3、KDR和Tie-2抑制剂弱(IC50>10uM)。

AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2. IC50 value: 5 nM Target: Src inhibitor in vitro: AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR . in vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection. Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight .

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Others

Other Targets

Others

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476159-98-5

442.94

C23H27ClN4O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 42 mg/mL (94.82 mM )

COc1ccc(Cl)c(Nc2ncnc3cc(OCC4CCN(C)CC4)c(OC)cc23)c1

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(-20℃)

With Ice Pack

≥ 2 years