THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC 50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression. Appearance:Solid IC50& Target:CDK7|3.2 nM (IC|50|)|CDK12|CDK13 In Vitro:THZ1 inhibits Jurkat cell and Loucy cell with IC 50 of 50 nM, and 0.55 nM, respectively. THZ1 demonstrates time-dependent inhibition of CDK7 in vitro and covalent binding of intracellular CDK7. THZ1 (9, 27, 83, 250, 750, and 2500 nM) inhibits CDK12 but at In Vivo:THZ1 (10mg/kg) demonstrates potent killing of primary chronic lymphocytic leukemia (CLL) cells and anti-proliferative activity against primary TALL cells and in vivo against a human T-ALL xenograft. THZ1 (10mg/kg, i.v.) inhibits tumor growth in a m Biological Activity:THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC 50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression .
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THZ1 Hydrochloride
CAS number：unknown molecular formula：C31H29Cl2N7O2
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compound introduction
Specs
| Chinese alias | THZ1盐酸盐 | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C31H29Cl2N7O2 |
| molecular weight | 602.51 g/mol | Exact mass | - |
| PSA | - | logp | - |
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