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THZ2 is a potent and selective CDK7 inhibitor with the potential to treat Triple-negative breast cancer. THZ2 at low nanomolar doses efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells.
In vivo, THZ2 (10 mg/Kg) markedly reduces the growth rate of tumors in mice and demonstrates an anti-tumor activity. THZ2 in NOD-SCID mice leads to reduced body weight, suggesting that THZ2 mayt be less well-tolerated in this particular mouse strain.
| Molecular Weight | 566.05 |
| Formula | C31H28ClN7O2 |
| CAS Number | 1604810-84-5 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Wang Y, et al. Cell. CDK7-dependent transcriptional addiction in triple-negative breast cancer.
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