产品
编 号：F533689
分子式：C25H28N6O2
分子量：444.53
分子式：C25H28N6O2
分子量：444.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 945755-56-6
产品详情
生物活性：
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
体内研究：
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?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
体内研究：
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.
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