QurientQ901 : highly selective CDK7 inhibitor


 

Q901 : highly selective CDK7 inhibitor

graph

Q901 is an extremely selective covalent CDK7 inhibitor showing potent tumor growth inhibition in high grade serous ovarian cancer and castration resistant prostate cancer. CDK7 is the master cell cycle regulator, acting on multiple cell cycle check points including CDK1, CDK2 and CDK4/6. It has a fundamental role in activation of CDK4/6 to phosphorylate retinoblastoma protein (RB) to facilitate early G1 prossion. In addition, CDK7 also can act on other check points(CDK1,CDK2), such it can regulate cell cycle even in case of RB pathway is altered and bypassing through other checkpoints.
Q901 is an extremely selective and potent CDK7 inhibitor. According to selectivity profiling panel test, the kinase with more 90% inhibition by Q901 is only CDK7 among 28 CDK/Cyclin complexes. Q901 shows potent tumor growth inhibition in high grade serous ovarian cancer(HGSOC) and castration resistant prostate cancer model(CRPC). Thses HGSOC and CRPC are one of the most serious cancer which are hard to treat with conventional therapy.
Q901 is under preclinical development with the first clinical study planned in 2021.

Poster

1. Highly selective, orally available CDK7 inhibitor for cancer therapy (2017 AACR-NCI-EORTC poster)
2. Development of highly selective CDK7 inhibitor Q901 for solid tumors (2020 AACR poster)

information for download file