ZT55

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

ZT55（JAK 抑制剂 ZT55）是一种新型强效、高选择性酪氨酸激酶 JAK2 抑制剂，IC50 为 31 nM。

ZT55 (JAK inhibitor ZT55) is a novel potent, highly-selective tyrosine kinase JAK2 inhibitor with IC50 of 31 nM; displays no significant activity against JAK1/3 (IC50>10 uM); exhibits potent effects on the cellular JAK-STAT pathway, inhibiting tyrosine phosphorylation in JAK2V617F and downstream STAT3/5 transcription factors; inhibits the proliferation of the JAK2V617F-expressing HEL cell line, leading to cell cycle arrest at the G2/M phase and induction of caspase-dependent apoptosis; significantly suppressed the growth of HEL xenograft tumors in vivo, blocks erythroid colony formation of peripheral blood hematopoietic progenitors from patients carrying the JAK2V617F mutation.

Cell Proliferation Assay Cell Line:HEL cells (JAK2V617F(+))Concentration:0-100 μM Incubation Time:48 h Result:Significantly inhibited proliferation in a concentration-dependent manner (IC50=18.05 μM).Cell Viability Assay Cell Line:HEL cells Concentration:12.5, 25, 50 μMIncubation Time:24, 48, 72 h Result:Inhibited viability of HEL cells in a concentration- and time-dependent manner.Apoptosis Analysis Cell Line:HEL cells (JAK2V617F(+))Concentration:0-100 μM Incubation Time:24, 48, 72 h Result:Induced cell apoptosis in a concentration- and time-dependent manner.Cell Cycle Analysis Cell Line:HEL cells (JAK2V617F(+))Concentration:0-100 μM Incubation Time:24, 48, 72 h Result:Significantly increased the number of HEL cells in the G2/M phase in a concentration-dependent manner.

Animal Model:Female, athymic BALB/c nude mice (6 to 8-week-old; JAK2V617F xenograft model).Dosage:100 mg/kg Administration:Oral administration; once a day for 2 weeks Result:Induced marked reductions in tumor volume.

JAK inhibitor ZT55

Angiogenesis

JAK

JAK

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2138488-38-5

296.326

C17H16N2O3

>98% (HPLC)

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2-(1-hydroxy-1H-indol-3-yl)-N-(2-methoxyphenyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years