SKLB 1028

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

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。

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.

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Animal Model:MV4-11 and K562 xenograft NOD-SCID modelsDosage: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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Angiogenesis

EGFR

EGFR | FLT | Bcr-Abl

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1350544-93-2

443.55

C24H29N9

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (563.63 mM; 超声助溶 )

C(C)(C)N1C=2C(N=C1NC=3C=CC=NC3)=CN=C(NC4=CC=C(C=C4)N5CCN(C)CC5)N2

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(-20℃)

With Ice Pack

≥ 2 years