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CC-671 是一种双重 TTK 蛋白激酶/CLK2抑制剂, 对于 TTK 和 CLK2 的IC50值分别为 0.005 和 0.006 μM。
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CC-671 是一种双重 TTK 蛋白激酶/CLK2抑制剂, 对于 TTK 和 CLK2 的IC50值分别为 0.005 和 0.006 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 495 | 现货 | |
5 mg | ¥ 1,160 | 现货 | |
10 mg | ¥ 1,890 | 现货 | |
25 mg | ¥ 3,820 | 现货 | |
50 mg | ¥ 5,550 | 现货 | |
100 mg | ¥ 7,770 | 现货 | |
500 mg | ¥ 15,500 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,290 | 现货 |
产品描述 | CC-671 is a dual TTK protein kinase (IC50: 0.005 μM) /CLK2 (IC50: 0.006 μM) inhibitor. |
靶点活性 | TTK:0.005 μM, CLK2:0.006 μM |
体外活性 | HCT-116细胞裂解物经3 μM的CC-671处理1小时后的结果表明,仅有四种激酶展示了75%或更高的细胞结合量,包括CLK2、CAMKK2、PIP4K22和JNK[1]。 |
体内活性 | CC-671在10mg/kg和20mg/kg剂量下,每3天给药一次的方案中显示出显著的肿瘤生长抑制效果,抑制率达71%((vehicle-treated/vehicle)×100%)。在20mg/kg剂量的CC-671处理组中,体重损失比10mg/kg组更高(17%对比5%)[1]。 |
激酶实验 | The kinase selectivity profile of CC-671 is assessed. The screen is conducted with the concentration of CC-671 held constant at 3 μM. The TTK binding affinity is measured using the kinase binding assays. The kinase binding assays are based on the binding and displacement of a proprietary, Alexa Fluor 647-labeled, ATP-competitive kinase inhibitor scaffold[1]. |
动物实验 | Female SCID mice are inoculated subcutaneously with 5×106 Cal-51 cells. Mice with tumours of approximately 125 mm3 are randomized and treated intravenously at various doses and schedules of CC-671 (n=8 to10/group). Tumours are measured twice a week for the duration of the study. The long and short axes of each a tumour are measured using a digital calliper in millimetres and the tumour volumes are calculated[1]. |
分子量 | 512.56 |
分子式 | C28H28N6O4 |
CAS No. | 1618658-88-0 |
Smiles | CNC(=O)c1ccc(Nc2nc(OC3CCCC3)c3c(c[nH]c3n2)-c2ccc3nc(C)oc3c2)c(OC)c1 |
密度 | 1.351 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (97.55 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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