RGB-286638

RGB-286638 is a small molecule, multi-targeted kinase inhibitor of the indenopyrazole family that primarily inhibits cyclin-dependent kinases (CDKs), including CDK1, CDK2, CDK4, CDK5, CDK6, and transcriptional kinases such as CDK7 and CDK9. It also inhibits several other cancer-relevant tyrosine and serine/threonine kinases such as GSK3β, TAK1, AMPK, JAK2, MEK1, FMS (CSF1R), c-Src and JNK isoforms. The drug acts by blocking cell cycle progression at both G1/S and G2/M phases and induces apoptosis in cancer cells through both p53-dependent and p53-independent mechanisms. Preclinical studies have shown efficacy in multiple myeloma models with both wild-type and mutant p53 status. In clinical development it has been evaluated for solid tumors in phase I trials; the recommended dose for further study was established at 120 mg/day intravenously for 5 days every 28 days[3][4][6][8]. The original developer was GPC Biotech AG; later development was led by Agennix AG[7].