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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 1895895-38-1 化合物 CHZ868
  • 化合物 CHZ868|TQ0061|TargetMol

化合物 CHZ868|TQ0061|TargetMol

CHZ868
1895895-38-1
￥657 2mg 起订
询价 50mg 起订
询价 5mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 CHZ868
英文名称：
CHZ868
CAS号：
1895895-38-1
品牌：
TargetMol
产地：
美国
保存条件：
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.38%
产品类别：
抑制剂
货号：
TQ0061

Product Introduction

Bioactivity

NameCHZ868
DescriptionCHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.
Cell ResearchCHZ868 is dissolved in DMSO to make 10 mM stock solution and diluted in culture media. Cells are treated with CHZ868 (0, 0.05, 0.1, 0.2 μM) or vehicle (DMSO). After 48 hr (Ba/F3 cells) or 72 hr (MHH-CALL4 and PDX cells), CellTiter-Glo Luminescent Cell Viability Assay is added (10 μL undiluted or 25 μL of a 1:2 dilution in each well) and plates are read [2].
Animal ResearchCHZ868 is reconstituted in 0.5% methylcellulose / 0.5% Tween-80 and administered at doses of 10 or 30 mg/kg/day by oral gavage. Pharmacokinetic/pharmacodynamic and efficacy studies in the mouse model of rhEpo-induced polycythemia are carried out essentially. Detection of STAT5 phosphorylation in spleen lysates by Meso Scale Discovery is performed [2].
In vitroCHZ868 effectively inhibits constitutive phosphorylation of JAK2 and STAT5 in JAK2V617F SET2 cells. The compound demonstrates potent inhibition of SET2 cell proliferation (GI50=59nM) and exhibits 6-fold lower growth inhibitory activity against CMK cells (GI50=378nM)[1]. At a concentration of 100 nM, CHZ868 shows activity against 26 kinases, including JAK2 and TYK2. It is believed that CHZ868 interacts with the hinge region of JAK2 through two hydrogen bonds, formed between the amino-pyridine of CHZ868 and the backbone-NH/CO of L932, while the pyridine occupies the adenine pocket of the ATP binding site. CHZ868 effectively suppresses the growth of CRLF2-rearranged human B-ALL cells and disrupts JAK2 signaling[1].
In vivoCharacterized by high passive permeability, good metabolic stability, and low water solubility, CHZ868 also exhibits moderate blood clearance and good oral bioavailability, rendering it suitable for in vivo applications. In mice with human or murine B-ALL, CHZ868 enhances survival. When used in combination with dexamethasone, CHZ868 synergistically induces apoptosis in JAK2-dependent B-ALLs, leading to improved survival compared to CHZ868 alone[1].
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 50 mg/mL (118.08 mM), Sonication is recommended.
KeywordsCHZ-868 | CHZ868 | CHZ 868
Inhibitors RelatedJAK-IN-10 | Tofacitinib Citrate | Deucravacitinib | RO8191 | Ruxolitinib | KW-2449 | TAK-901 | CEP-33779 | Baricitinib | Fedratinib | Ruxolitinib phosphate | Delgocitinib
CHZ868|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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