SKLB 1028

Research use only, not for human use.

SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants.

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 : 250 mg/mL (563.63 mM; Ultrasonic )

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