化合物 CHZ868|TQ0061|TargetMol

價格	￥343	￥506
包裝	1mg	2mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2025-07-28

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產(chǎn)品詳情

中文名稱:化合物 CHZ868	英文名稱:CHZ868
CAS:1895895-38-1	品牌: TargetMol
產(chǎn)地: 美國	保存條件: store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.38%	產(chǎn)品類別: 抑制劑
貨號: TQ0061

Product Introduction

Bioactivity

名稱	CHZ868
描述	CHZ868 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.
細(xì)胞實驗	CHZ868 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].
動物實驗	CHZ868 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].
體外活性	CHZ868 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].
體內(nèi)活性	Characterized 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].
存儲條件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (118.08 mM), Sonication is recommended.
關(guān)鍵字	JAK2 \| JAK1 \| CHZ-868 \| CHZ868 \| CHZ 868
相關(guān)產(chǎn)品	JAK-IN-10 \| Fedratinib \| Upadacitinib \| Tofacitinib Citrate \| Deucravacitinib \| RO8191 \| KW-2449 \| TAK-901 \| CEP-33779 \| Baricitinib \| Ruxolitinib phosphate \| Delgocitinib

關(guān)鍵字： CHZ868|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計算機(jī)輔助藥物設(shè)計）研究中心、藥理實驗室、藥化合成平臺三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （13年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：13年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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