化合物GZD824 Dimesylate T2429
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
50 mg | 1421783-64-3 | ¥3,920.00 | 询底价 |
25 mg | 1421783-64-3 | ¥2,490.00 | 询底价 |
10 mg | 1421783-64-3 | ¥1,230.00 | 询底价 |
100 mg | 1421783-64-3 | ¥5,580.00 | 询底价 |
1 mg | 1421783-64-3 | ¥329.00 | 询底价 |
5 mg | 1421783-64-3 | ¥788.00 | 询底价 |
1 mL | 1421783-64-3 | ¥1,250.00 | 询底价 |
2 mg | 1421783-64-3 | ¥478.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Olverembatinib dimesylate
描述: Olverembatinib dimesylate (GZD824 Dimesylate) 是一种高效的、口服具有活性的pan-Bcr-Abl 抑制剂,具有抗肿瘤活性。它能广泛而有效地抑制突变型 Bcr-Abl。它对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的IC50值分别为 0.34 nM 和 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: 每天20 mg/kg GZD824抑制表达的Bcr-AblWT和BCR-AblT315I的Ba/F3细胞的同种异体移植小鼠中肿瘤生长.每天5和10 mg/kg GZD824剂量依赖性地抑制了K562肿瘤异种移植物和KU812异种移植模型中肿瘤的生长,并且没有死亡或体重减轻.
体内活性: GZD824以浓度依赖性方式有效抑制白血病细胞中Bcr-Abl以及下游Crk1和STAT5的活化。与生化激酶抑制和蛋白质结合亲和力实验结果高度相符,GZD824也强烈抑制表达Bcr-AblT315I突变体和其他14个与抗性有关的Bcr-Abl突变体的Ba/F3细胞的增殖。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 92 mg/mL (126.9 mM)
DMSO : 93 mg/mL (128.3 mM)
关键字: region-Abelson | phosphorylated | imatinib | Olverembatinib dimesylate | inhibit | linase | Inhibitor | HQP-1351 | nonphosphorylated | breakpoint | resistance | GZD-824 Dimesylate | HQP 1351 | HQP1351 dimesylate | Olverembatinib Dimesylate | GZD 824 Dimesylate | GZD-824 | GZD824 | Bcr-Abl | Bcr-Abl(T315I) | GZD 824 | cluster | Olverembatinib
相关产品: CpCDPK1/TgCDPK1-IN-1 | PD180970 | Imatinib impurities3 | PD173955 | Asciminib | Agerafenib | GMB-475 | URMC-099 | Lyn-IN-1 | Dasatinib
相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途