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ZT55
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZT55图片
CAS NO:2138488-38-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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].

IC50& Target[1]

JAK2

0.031 μM (IC50)

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.
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.
分子量

296.32

Formula

C17H16N2O3

CAS 号

2138488-38-5

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.