HQY1428

HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect[1].

C25H28ClFN6O3S

547.04

O=S(C1=C(C=CC=C1)NC2=C(C=NC(N[C@@H]3CCCN(C3)C(C4=CC(F)=CC(N)=C4)=O)=N2)Cl)(C(C)C)=O

Apoptosis; CDK; DNA/RNA Synthesis

CDK12

99.65

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature