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Ruserontinib

CAS No. : 1350544-93-2

MCE 国际站：Ruserontinib

产品活性：Ruserontinib (SKLB1028)是一种具有口服活性的 EGFR、FLT3 和Abl 多激酶抑制剂，作用于人FLT3 的 IC₅₀ 值为 55 nM，具有抗肿瘤活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR  |  FLT3  |  Bcr-Abl

In Vitro: Ruserontinib (SKLB1028) can significantly inhibit the growth of mf4-11 cells expressing FLT3-ITD with IC₅₀ value of 0.002 μM, inhibit the proliferation of RS4-11 cells expressing wt-FLT3 with IC₅₀ value of 0.790 μM, and inhibit Ba The IC₅₀ value for the growth of /F3 cells is 0.01 μM, and the IC₅₀ value for inhibiting the growth of K562 cells expressing the Bcr-Abl mutant is 0.190 μM.
Ruserontinib (SKLB1028) (0-100 nM, 20 h) causes a dose-dependent decrease in the level of pro-caspase-3 in MV4-11 cells, while a dose-dependent increase in the level of the cleaved caspase-3 fragment, and can be dose-dependent Inhibits phosphorylation of STAT5 and Erk1/2 in a dependent manner.

In Vivo: Ruserontinib (SKLB1028) (5-70 mg/kg, orally once daily, 18 days) have anti-tumor effect in MV4-11 and K562 xenograft NOD-SCID models.

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