Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 329 | 现货 | ||
2 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,920 | 现货 | ||
100 mg | ¥ 5,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,250 | 现货 |
产品描述 | Olverembatinib dimesylate (GZD824 Dimesylate) is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I). |
靶点活性 | Abl (M351T):0.29 nM, Abl (H396P):0.35 nM, Abl:0.34 nM, Abl (Q252H):0.15 nM, Abl (E255K):0.27 nM |
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。 |
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. |
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) |
别名 | GZD824 Dimesylate, HQP1351 |
分子量 | 724.77 |
分子式 | C29H27F3N6O·2CH4O3S |
CAS No. | 1421783-64-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 92 mg/mL (126.9 mM)
DMSO: 93 mg/mL (128.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 1.3797 mL | 6.8987 mL | 13.7975 mL | 34.4937 mL |
5 mM | 0.2759 mL | 1.3797 mL | 2.7595 mL | 6.8987 mL | |
10 mM | 0.138 mL | 0.6899 mL | 1.3797 mL | 3.4494 mL | |
20 mM | 0.069 mL | 0.3449 mL | 0.6899 mL | 1.7247 mL | |
50 mM | 0.0276 mL | 0.138 mL | 0.2759 mL | 0.6899 mL | |
100 mM | 0.0138 mL | 0.069 mL | 0.138 mL | 0.3449 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Olverembatinib dimesylate 1421783-64-3 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl region-Abelson phosphorylated imatinib GZD824 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(T315I) GZD 824 HQP1351 cluster Olverembatinib inhibitor