XL019

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

XL019 是一种有效的选择性 JAK2 抑制剂，IC50 为 2.2 nM。

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1.(In Vivo):XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth.XL019 (10 mg/kg) treatment shows that the Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, 5.319 L/kg, respectively.

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XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth.XL019 (10 mg/kg) treatment shows that the?Cmax, t1/2?and Vd were?5.24 μM,?1.94 hours,?5.319 L/kg,?respectively. Animal Model:Female nude mice (HEL.92.1.7 xenograft tumors)Dosage:100, 200, 300 mg/kg Administration:p.o.; twice daily for 14 days Result:Inhibition of HEL.92.1.7 xenograft tumor growth.Animal Model:Mouse Dosage:10 mg/kg Administration:p.o.(Pharmacokinetic?Analysis)Result:The?Cmax, t1/2?and Vd were?5.24 μM,?1.94 hours,?and 5.319 L/kg,?respectively.

XL019 | XL-019 | XL 019

Angiogenesis

FLT

FLT3| JAK1| JAK2| JAK3| PDGFRβ

Cancer

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945755-56-6

444.53

C25H28N6O2

>98% (HPLC)

DMSO: 16 mg/mL (35.99 mM)

O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2

(S)-N-(4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years