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CDK8-IN-12 是一种具有选择性、有效性和口服活性的 CDK8 抑制剂(Ki : 14 nM),是一种抗癌剂。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有抑制作用,Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12对 MV4-11 细胞显示出抗增殖活性。


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CDK8-IN-12 是一种具有选择性、有效性和口服活性的 CDK8 抑制剂(Ki : 14 nM),是一种抗癌剂。CDK8-IN-12 对 GSK-3α、GSK-3β、PCK-θ 具有抑制作用,Ki 分别为 13 nM、4 nM、109 nM。CDK8-IN-12对 MV4-11 细胞显示出抗增殖活性。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 311 | In stock | |
| 5 mg | ¥ 713 | In stock | |
| 10 mg | ¥ 1,070 | In stock | |
| 25 mg | ¥ 1,780 | In stock | |
| 50 mg | ¥ 2,680 | In stock | |
| 100 mg | ¥ 3,760 | In stock | |
| 200 mg | ¥ 5,080 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 762 | In stock |
CDK8-IN-12 相关产品
| 产品描述 | CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells. |
| 靶点活性 | MV-4-11 cells:0.36 μM(GI50), GSK-3β:4 nM(ki), PCKθ:109 nM(ki), GSK-3α:13 nM(ki), CDK8:14 nM(Ki) |
| 体外活性 | CDK8-IN-12 (0.36, 0.72 μM ; 2 h) significantly reduced the phosphorylation of STAT1 serine 727.[1] |
| 体内活性 | CDK8-IN-12 (intravenous administration ; 5 mg/kg in rats ; 2 mg/kg in mice) had a T1/2 of 0.9 h and 0.34 h in rats and mice, respectively.[1] |
| 分子量 | 381.86 |
| 分子式 | C21H20ClN3O2 |
| CAS No. | 2613307-67-6 |
| Smiles | O=C1C2(CCN(CC2)C=3C(=CN=CC3Cl)C4=CC=5C(O4)=CC=CC5)CCN1 |
| 密度 | 1.39 g/cm3 at 20℃ (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 27.5 mg/mL (72.02 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.24 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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