Powder: -20°C for 3 years | In solvent: -80°C for 1 year
3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | 待询 | 待询 | ||
500 mg | 待询 | 待询 |
产品描述 | 3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy. |
靶点活性 | CDK4:0.11 μM (IC50), GSK-3:41 nM (IC50), CDK2-CyclinA:2 nM (IC50), FGFR2:0.22 μM (IC50), CDK1-CyclinB:6.4 nM (IC50), VEGFR2:0.13 μM (IC50) |
体外活性 | 3-Methylthienyl-carbonyl-JNJ-7706621 shows potent potency against GSK-3 (IC 50 =0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC 50 =0.11, 0.13, 0.22 μM, respectively)[1]. 3-Methylthienyl-carbonyl-JNJ-7706621 inhibits cell proliferation, with IC 50 s of 0.28 μM, 0.25 μM, 0.45 μM, 0.75 μM, 0.59 μM and 0.12 μM for HeLa, HCT-116, A375, SK-OV-3, MDA-MB-231 and PC-3 cells, respectively[1]. |
体内活性 | 3-Methylthienyl-carbonyl-JNJ-7706621 (75-125 mg/kg; i.p. once daily for 32 days) inhibits the A375 human melanoma tumor growth and prolongs the survival in nude mice[1]. 3-Methylthienyl-carbonyl-JNJ-7706621 exhibits oral bioavailability (nude mouse 2%, rat 8%, dog 63.3%), terminal elimination half-lives (nude mouse 1.70, rat 2.20 and, dog 2.36 h) and C max (nude mouse 0.21, rat 2.5, dog 4.58 μM) following oral administration (nude mouse 30, rat 30 , dog 10 mg/kg)[1]. 3-Methylthienyl-carbonyl-JNJ-7706621 exhibits terminal elimination half-lives (nude mouse 0.51, rat 0.64 and, dog 3.89 h), C max (nude mouse 6.4, rat 23.2, dog 2.19 μM) and AUC (nude mouse 3.2, rat 11.4, dog 2.45 μM?h) following intravenous administration (nude mouse 3, rat 3 and, dog 1 mg/kg)[1]. Animal Model: Male athymic mice were implanted with A375 human melanoma cells[1]Dosage: 75, 100, 125 mg/kg Administration: I.p. once daily for 32 days Result: Reduced the tumor growth. Survival was increased by about 3 weeks compared with vector alone. |
分子量 | 378.43 |
分子式 | C14H14N6O3S2 |
CAS No. | 443798-09-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
3-Methylthienyl-carbonyl-JNJ-7706621 443798-09-2 3-Methylthienyl-carbonyl-JNJ 7706621 3-Methylthienyl-carbonyl-JNJ7706621 3 Methylthienyl carbonyl JNJ 7706621 3MethylthienylcarbonylJNJ7706621 Inhibitor inhibitor inhibit