【CAS No.】 571190-30-2
【Formula 】C10H11N3O3S
【GMP National Medicine Permission Number】
【Drug Class】 Antineoplastic
【Formulation Use】 Palbociclib Capsule
【Packing Specification】10kg/Barrel
【Standard】 CP, EP,USP,BP ,ect
【Description】: Palbociclib, sold under the brand name Ibrance among others, for the treatment of HR-positive and HER2-negative breast cancer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Palbociclib was the first CDK4/6 inhibitor to be approved as a cancer therapy.
Mechanism of action
Further information: CDK inhibitor
It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.
In the G1 phase of the cell cycle, mammalian cells must pass a checkpoint, known as the restriction point "R", in order to complete the cell cycle and divide. CDK4 and CDK6 complex with cyclin D drive the phosphorylation of the retinoblastoma protein, Rb, which allows the cell to pass R and commit to division. Regulation of one or more proteins involved in this checkpoint is lost in many cancers. However, by inhibiting CDK4/6, palbociclib ensures that the cyclin D-CDK4/6 complex cannot aid in phosphorylating Rb. This prevents the cell from passing R and exiting G1, and in turn from proceeding through the cell cycle.