ZT55 是一种口服有效并具有高选择性的JAK2抑制剂，其IC50值为 0.031 μM。ZT55 能抑制表达JAK2V617F的 HEL 细胞系的增殖，并诱导细胞凋亡和周期停滞。ZT-55 还可有效抑制小鼠模型体内 HEL 异种移植肿瘤的生长。ZT-55 可用于骨髓增生性肿瘤、多血症以及原发性血小板增多症的研究。
| 生物活性 | ZT55 is an orally active and highly-selectiveJAK2inhibitor with anIC50value of 0.031 μM. ZT55 inhibits the proliferation ofJAK2V617F-expressing HEL cell lines and inducesapoptosisand cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia[1]. |
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体外研究
(In Vitro) | ZT55 (0-100 μM; 48 h) 以浓度依赖的方式对 JAK2V617F表达阳性的 HEL 细胞显示抗增殖活性 (IC50=18.05 μM)[1]。
ZT55 (12.5, 25, 50 μM; 24, 48, 72 h) 以浓度和时间依赖的方式抑制 HEL 细胞的活力并诱导细胞凋亡[1]。
ZT55 (12.5, 25, 50 μM; 24 h) 以浓度依赖的方式诱导 HEL 细胞阻滞在 G2/M 期[1]。
Cell Proliferation Assay[1] | 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[1] | Cell Line: | HEL cells | | Concentration: | 12.5, 25, 50 μM | | Incubation Time: | 24, 48, 72 h | | Result: | Inhibited viability of HEL cells in a concentration- and time-dependent manner. |
Apoptosis Analysis[1] | 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[1] | 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. |
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体内研究
(In Vivo) | ZT55 (100 mg/kg; p.o; once a day for 2 weeks) 显著抑制裸鼠皮下 HEL 肿瘤的生长[1]。
| Animal Model: | Female, athymic BALB/c nude mice (6 to 8-week-old; JAK2V617Fxenograft model)[1]. | | Dosage: | 100 mg/kg | | Administration: | Oral administration; once a day for 2 weeks | | Result: | Induced marked reductions in tumor volume. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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