keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TL12-186 是一种依赖于 Cereblon 的激酶降解剂,可降解 CDK,BTK,FLT3,Aurora 等激酶。TL12-186 对 CDK2/cyclin A 和 CDK9/cyclin T1 有抑制作用,IC50 分别为 73 和 55 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,150 | 现货 | ||
5 mg | ¥ 2,880 | 现货 | ||
10 mg | ¥ 4,890 | 现货 | ||
25 mg | ¥ 7,470 | 现货 | ||
50 mg | ¥ 9,870 | 现货 | ||
100 mg | ¥ 13,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,910 | 现货 |
产品描述 | TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively. |
靶点活性 | CDK2-CyclinA:73 nM (IC50), CRBN:12nM, CDK9-CyclinT1:55 nM (IC50) |
体外活性 | TL12-186 demonstrates over 90% inhibition against 193 kinases at a screening concentration of 1 μM[1]. Utilizing AlphaScreen binding assays, it exhibits potent binding to CRBN with an IC50 of 12 nM[1]. Displaying CRBN-dependent pharmacological effects, TL12-186 (1-10000 nM; 2 days) exerts 13 to 15 times stronger inhibition of cell survival in WT cells compared to CRBN-/- cells[1]. Moreover, at concentrations ranging from 10 to 10000 nM for 4 hours, TL12-186 selectively inhibits STAT1 phosphorylation without inducing degradation of JAK1/2[1]. |
别名 | TL12 186, TL12186 |
分子量 | 931.46 |
分子式 | C44H51ClN10O9S |
CAS No. | 2250025-88-6 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (214.72 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0736 mL | 5.3679 mL | 10.7358 mL | 26.8396 mL |
5 mM | 0.2147 mL | 1.0736 mL | 2.1472 mL | 5.3679 mL | |
10 mM | 0.1074 mL | 0.5368 mL | 1.0736 mL | 2.684 mL | |
20 mM | 0.0537 mL | 0.2684 mL | 0.5368 mL | 1.342 mL | |
50 mM | 0.0215 mL | 0.1074 mL | 0.2147 mL | 0.5368 mL | |
100 mM | 0.0107 mL | 0.0537 mL | 0.1074 mL | 0.2684 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。
TL12-186 2250025-88-6 Cell Cycle/Checkpoint PROTAC CDK Ligand for E3 Ligase TL 12186 TL12 186 TL12186 TL-12186 Inhibitor inhibitor inhibit