SR-4835 是有效，高选择性和 ATP 竞争性的 CDK12/CDK13 双重抑制剂 (CDK12:IC50=99 nM，Kd=98 nM；CDK13:Kd=4.9 nM)。SR-4835 与破坏 DNA 的化学疗法和 PARP 抑制剂协同作用，并引起三阴性乳腺癌 (TNBC) 细胞凋亡。
| Cas No. | 2387704-62-1 |
| Canonical SMILES | CN1N=CC(N2C3=NC(N4CCOCC4)=NC(NCC5=NC6=C(N5)C=C(Cl)C(Cl)=C6)=C3N=C2)=C1 |
| 分子式 | C21H20Cl2N10O |
| 分子量 | 499.36 |
| 溶解度 | DMSO: 5 mg/mL (10.01 mM; ultrasonic and warming and heat to 60℃) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death[1]. [1]. Quereda V, et al. Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer. Cancer Cell. 2019 Oct 8. pii: S1535-6108(19)30424-6. |
