Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fadraciclib (CYC065) 是一种口服有效的 ATP 竞争性的CDK2/CDK9激酶抑制剂,IC50分别为 5 和 26 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,830 | 现货 | ||
10 mg | ¥ 4,180 | 现货 | ||
25 mg | ¥ 6,720 | 现货 | ||
50 mg | ¥ 9,120 | 现货 | ||
100 mg | ¥ 12,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,120 | 现货 |
产品描述 | Fadraciclib (CYC065) is an orally available, second-generation ATP-competitive inhibitor of CDK2/CDK9 kinases (IC50s: 5/26 nM). |
靶点活性 | CDK9:26 nM, CDK2:5 nM |
体外活性 | CYC065通过阻碍细胞在细胞周期G1阶段的活动,并特异性抑制在环形蛋白E1 (CCNE1) 过表达的子宫浆液性癌症(USCs)中的细胞生长。与低CCNE1表达的细胞系相比,高CCNE1 mRNA及蛋白水平的USC细胞系对CYC065的治疗表现出更高的敏感性(IC50: 平均±标准差=124.1±57.8nM 对CCNE1过表达的USC细胞系 vs 415±117.5nM 对CCNE1低表达者;P=0.0003)。重要的是,低浓度的CYC065(即,100nM)仅在CCNE1过表达的USC细胞系中引起细胞周期G1阶段的停滞[1]。 |
体内活性 | USC-ARK-2衍生的异种移植物每日使用CYC065 (22.5 mg/kg)治疗共3周。肿瘤大小与小鼠体重每周记录两次。CYC065的日常给药显著减缓了与对照组相比的肿瘤生长(治疗第9天起,P=0.012)。整个治疗期间未报告有显著的体重减轻[1]。 |
细胞实验 | Briefly, tumour cells are plated in six-well plates and treated with a titration of CYC065 concentrations (i.e., ranging from 100 to 500?nM). After 72?h, cells are harvested, washed and stained with propidium iodide (PI; 5?μg/mL) for flow cytometric counts. The percentage of viable cells is then normalized considering the vehicle-treated cells as 100% viable. Half-maximal inhibitory concentration values are determined using GraphPad Prism5 version 6. For drug combination studies, USC-ARK-1 and USC-ARK-2 cell lines are incubated with the combination of Taselisib and CYC065 at multiple paired concentrations including the IC50, the IC50/2 and the IC50*2 of each cell line to the corresponding drug (i.e., 10?nM of Taselisib and 198?nM of CYC065 for USC-ARK-1 and 50?nM of Taselisib and 62.5?nM of CYC065 for USC-ARK-2). Synergism is assessed by the combination index (CI). CI values <1 define a synergistic activity of the combination treatment. The CI values are calculated using the CompuSyn software [1]. |
动物实验 | Briefly, 5-7-week-old SCID mice are injected into the subcutaneous region with USC cells. A minimum of five animals per group are used. Treatments are administrated by oral gavage starting 1 week after tumor implantation when the size of the tumor is 0.125-0.150?cm3. Uterine serous carcinoma-ARK-2-derived xenografts are divided into two groups: one group of animal receive the vehicle, whereas the experimental group receives CYC065 (22.5?mg/kg daily for 3 weeks). Uterine serous carcinoma-ARK-1-derived xenografts are instead divided into four groups: one group receive the vehicle (0.5% methylcellulose-0.2% Tween-80), one group receive CYC065 (22.5?mg/kg daily for 3 weeks), one group receive Taselisib (10 mg/kg daily, 5 days per week per 3 weeks) and the last group receive the combination of CYC065 and Taselisib. The size of the tumor at the initiation of treatment is 0.125-0.150?cm3. Mouse weight and tumor size is recorded two times a week for the entire experimental period. Tumor volume is calculated. |
别名 | CYC065 |
分子量 | 397.52 |
分子式 | C21H31N7O |
CAS No. | 1070790-89-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (251.56 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5156 mL | 12.578 mL | 25.156 mL | 62.8899 mL |
5 mM | 0.5031 mL | 2.5156 mL | 5.0312 mL | 12.578 mL | |
10 mM | 0.2516 mL | 1.2578 mL | 2.5156 mL | 6.289 mL | |
20 mM | 0.1258 mL | 0.6289 mL | 1.2578 mL | 3.1445 mL | |
50 mM | 0.0503 mL | 0.2516 mL | 0.5031 mL | 1.2578 mL | |
100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6289 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。
Fadraciclib 1070790-89-4 Cell Cycle/Checkpoint CDK Cyclin dependent kinase Inhibitor CYC 065 CYC-065 inhibit CYC065 inhibitor