| Description |
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].
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| Related Catalog |
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| In Vitro |
Ruserontinib (SKLB1028)可以显著抑制表达 FLT3-ITD的 mf4 -11 细胞的生长，IC50值为 0.002 μM，抑制表达 wt-FLT3 的 RS4-11 细胞增殖的 IC50值为 0.790 μM，抑制稳定表达人 FLT3ITD 的 Ba/F3 细胞生长的IC50值为 0.01 μM，抑制表达 Bcr-Abl 突变体的 K562 细胞生长的 IC50为0.190 μM[1]。 Ruserontinib (SKLB1028) (0-100 nM, 20 h)导致 MV4-11 细胞的 pro-caspase-3水平呈剂量依赖性下降，而被切割的 caspase-3 片段水平呈剂量依赖性增加，并且可以以剂量依赖的方式抑制 STAT5 和 Erk1/2 的磷酸化[1]。
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| In Vivo |
Ruserontinib (SKLB1028)（5-70 mg/kg，每天口服一次，18 天）在 MV4-11 和 K562 异种移植 NOD-SCID 模型中具有抗肿瘤作用[1]。 Animal Model: MV4-11 and K562 xenograft NOD-SCID models[1] Dosage: 5, 10, 20 mg/kg,70 mg/kg Administration: orally once daily, 18 days Result: Prevented tumor growth at a dose of 5 mg/kg, and caused rapid and complete tumor regression in both groups of mice at a dose of 10 or 20 mg/kg. Significantly inhibited the proliferation and induced apoptosis of MV4-11 and K562 cells at a dose of 70 mg/kg.
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| References |
[1]. Z-X Cao, et al. SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants. Leukemia. 2012 Aug;26(8):1892-5.
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