化合物 GZD 824|T3071|TargetMol

Olverembatinib
1257628-77-5

￥248 1mg 起订

￥368 2mg 起订

￥645 5mg 起订

上海更新日期：2025-11-17

TargetMol中国（陶术生物）

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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 GZD 824

英文名称：: Olverembatinib

CAS号：: 1257628-77-5

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：: 99.29%

产品类别：: 抑制剂

货号：: T3071

Product Introduction

Bioactivity

名称	Olverembatinib
描述	Olverembatinib (GZD 824) is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
细胞实验	Cells in the logarithmic phase are plated in 96-well culture dishes. Twenty-four hours later, cells are treated with the corresponding compounds or vehicle control at the indicated concentration for 72 h. CCK-8 is added into the 96-well plates (10 μL/well) and incubated with the cells for 3 h. OD450 and OD650 are determined by a microplate reader. Absorbance rate (A) for each well is calculated as OD450 – OD650. The cell viability rate for each well is calculated as V% = (As – Ac)/(Ab – Ac) × 100%, and the data were further analyzed using Graphpad Prism5. The data are the mean value of the three experiments. As is the absorbance rate of the test compound well, Ac is the absorbance rate of the well without either cell or test compound, and Ab is the absorbance rate of the well with cell and vehicle control.(Only for Reference)
激酶实验	FRET-Based Z′-Lyte Assay Detecting Peptide Substrate Phosphorylation: The kinases ABL1, ABL1(E255K), ABL1 (G250E), ABL1(T315I), and ABL1(Y253F) are P3049, PV3864, PV3865, PV3866, and PV3863 are full-length human recombinant protein expressed in insect cells and histidine-tagged. Inhibition activities of inhibitors against Abl1 and its mutants are performed in 384-well plates using the FRET-based Z′-Lyte assay system. Briefly, the kinase substrate is diluted into 5 μL of kinase reaction buffer; and the kinase is added. Compounds (10 nL) with indicated concentrations are then delivered to the reaction by using Echo liquid handler, and the mixture is incubated for 30 min at room temperature. Then 5 μL of 2X ATP solution is added to initiate the reaction, and the mixture is further incubated for 2 h at room temperature. The resulting reactions contains 10 μM (for wild-type Abl1, and mutants Y253F, Q252H, M351T, and H396P) or 5 μM (for mutants E255K, G250E, T315I) of ATP, 2 μM of Tyr2 Peptide substrate in 50 mM HEPES (PH 7.5), 0.01% BRIJ-35, 10 mM MgCl2, 1 mM EGTA, 0.0247 μg/mL Abl1, and inhibitors as appropriate. Then, 5 μL of development reagent is added, and the mixture is incubated for 2 h at room temperature before 5 μL of stop solution is added. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) is examined on an EnVision Multilabel Reader. The data are analyzed using Graphpad Prism5. The data are the mean value of three experiments.
体外活性	Olverembatinib 强效抑制表达野生型 Bcr-Abl 的 Ba/F3 细胞增长，IC50 为 1.0 nM。与生化激酶抑制和紧密蛋白结合亲和力高度一致，Olverembatinib 也强烈抑制表达 Bcr-AblT315I 突变体及其他 14 种抗性相关 Bcr-Abl 突变体的 Ba/F3 细胞增殖。此外，Olverembatinib 在浓度依赖的方式下有效抑制 K562 CML 细胞中 Bcr-Abl 及其下游 Crkl 和 STAT5 的活化。[1]
存储条件	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 : 100 mg/mL (187.77 mM), Sonication is recommended.
关键字	resistance \| region-Abelson \| phosphorylated \| Olverembatinib \| nonphosphorylated \| linase \| Inhibitor \| inhibit \| imatinib \| HQP-1351 \| HQP1351 \| HQP 1351 \| GZD-824 \| GZD824 \| cluster \| breakpoint \| Bcr-Abl(T315I) \| Bcr-Abl \| BcrAbl \| Abl (E254K)
相关产品	Ponatinib \| Pivanex \| Imatinib \| Bosutinib hydrate \| KW-2449 \| Masitinib \| Vodobatinib \| Nilotinib monohydrochloride monohydrate \| Bosutinib \| GNF-5 \| Dasatinib \| Nilotinib
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 临床前化合物库 \| 临床期小分子药物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

奥雷巴替尼|||GZD 824|TargetMol

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。

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