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Chemical Structure : THZ1
CAS No.: 1604810-83-4
Catalog No.: PC-46008Not For Human Use, Lab Use Only.
THZ1 is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM, also weakly inhibits CDK12 with IC50 of 250 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | Get quote |
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THZ1 is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM, also weakly inhibits CDK12 with IC50 of 250 nM.
THZ1 displays broad-based activity a subset of cancer cell lines with IC50s of <200 nM.
THZ1 causes decreased cellular proliferation and an increase in apoptotic index (MCL-1, XIAP), disproportionally affects transcription of RUNX1 in Jurkat T-ALL cells.
THZ1 demonstrates efficacy against primary leukemia cells and in a bioluminescent xenografted model at 10mg/kg.
| M.Wt | 566.0527 | |
| Formula | C31H28ClN7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 27 mg/mL |
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| Chemical Name/SMILES |
Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]- |
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1. Kwiatkowski N, et al. Nature. 2014 Jul 31;511(7511):616-20.
2. Chipumuro E, et al. Cell. 2014 Nov 20;159(5):1126-39.
3. Christensen CL, et al. Cancer Cell. 2014 Dec 8;26(6):909-22.
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