THZ1 Hydrochloride

THZ1盐酸盐

THZ1 Hydrochloride

T658911-5mg

5mg

Moligand™

≥98%

2-8°C储存,干燥

冰袋运输

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 .

C31H29Cl2N7O2

602.51 g/mol

ClC1=CN=C(NC2=CC(NC(C3=CC=C(NC(/C=C/CN(C)C)=O)C=C3)=O)=CC=C2)N=C1C4=CNC5=CC=CC=C54.Cl

DMSO : 22.5 mg/mL (37.34 mM; Need ultrasonic and warming) H2O : ＜ 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)