RGB-286638 free base

Description	RGB-286638 inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. RGB-286638 demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manifesting less cytotoxicity in healthy donor PBMCs. Treatment with RGB-286638 resulted in rapid downregulation of p-RNAPII S2/S5 across all tested MM cell lines. RGB-286638 (50nM) reduced the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but had no effects on p-Rb S780. in vivo: Dose-finding studies with RGB-286638 identified 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppressed MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively.
Pathways	Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Jak/Stat Pathway Wnt/Stem Cell PI3K/Akt/mTOR MAPK Pathway Epigenetics
Targets	MEK/ERK GSK3 JAK CDK

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