货号	规格	价格	上海	北京	珠海	重庆	武汉
S84139-5mg	≥98%	￥780.00 S84139-5mg ￥780.00 3-5天	0 货期：3-5天	-	-	-	-
S84139-10mg	≥98%	￥1090.00 S84139-10mg ￥1090.00 3-5天	0 货期：3-5天	-	-	-	-
S84139-25mg	≥98%	￥1970.00 S84139-25mg ￥1970.00 3-5天	0 货期：3-5天	-	-	-	-
S84139-50mg	≥98%	￥3410.00 S84139-50mg ￥3410.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

靶点：

JAK2:110 nM (IC50);JAK

体外研究：

CHZ868 potently inhibits constitutive JAK2 and STAT5 phosphorylation in JAK2V617F SET2 cells. CHZ868 potently inhibits the proliferation of SET2 cells (GI50=59nM), and has 6-fold less growth inhibitory activity against CMK cells (GI50=378nM). At 100 nM CHZ868 has activity against 26 kinases, including JAK2 and TYK2. CHZ868 is thought to engage with the hinge region of JAK2 through two H-bonds, formed between the amino-pyridine of CHZ868 and the backbone-NH/CO of L932, while the pyridine is occupying the adenine pocket of the ATP binding site. CHZ868 potently suppresses the growth of CRLF2-rearranged human B-ALL cells, abrogates JAK2 signaling

体内研究：

CHZ868 is characterized by high passive permeability, good metabolic stability, and low water solubility, as well as by moderate blood clearance and good oral bioavailability, making it suitable for in vivo use. CHZ868 improves survival in mice with human or murine B-ALL. CHZ868 and dexamethasone synergistically induces apoptosis in JAK2-dependent B-ALLs and further improves survival compared to CHZ868 alone

参考文献：

1. Meyer SC, et al. CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms. Cancer Cell. 2015 Jul 13;28(1):15-28. 2. Wu SC, et al. Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia. Cancer Cell. 2015 Jul 13;28(1):29-41.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.362 ml	11.809 ml	23.617 ml
5 mM	0.472 ml	2.362 ml	4.723 ml
10 mM	0.236 ml	1.181 ml	2.362 ml
50 mM	0.047 ml	0.236 ml	0.472 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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