Chemical Structure : THZ2
CAS No.: 1604810-84-5
Catalog No.: PC-42944Not For Human Use, Lab Use Only.
THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1.
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THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1.
THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells, efficiently suppresses the clonogenic growth of TNBC cells with IC50 of 10 nM.
Like THZ1, THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells.
THZ2 suppresses the growth of triple-negative breast tumors in xenograft models.
M.Wt | 566.0527 | |
Formula | C31H28ClN7O2 | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: ≥ 39 mg/mL |
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Chemical Name/SMILES |
Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-3-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]- |
1. Wang Y, et al. Cell. 2015 Sep 24;163(1):174-86.
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