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3-Methylthienyl-carbonyl-JNJ-7706621

产品编号 T40546 CAS 443798-09-2

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.

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3-Methylthienyl-carbonyl-JNJ-7706621 Chemical Structure

3-Methylthienyl-carbonyl-JNJ-7706621, CAS 443798-09-2

规格	价格/CNY		货期	数量
100 mg	待询		待询
500 mg	待询		待询

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参考文献

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Lin R, et, al. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.

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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。

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