Flavopiridol hydrochloride

A potent, ATP-competetive CDKs inhibitor with IC50 of 30, 170, 100 nM for CDk1, 2, 4, respectively; inhibits cell cycle progression in either G1 or G2 in human breast carcinoma cells, induces programmed cell death, promote differentiation, inhibits angiogenic processes and modulates transcriptional events.Blood Cancer Phase 2 Clinical (In Vitro) :Flavopiridol (2 μM) robustly induces a distinct pattern of ER stress in CLL cells that contributes to cell death through IRE1-mediated activation of ASK1 and possibly downstream caspases. Flavopiridol results in potent upregulation of a number of PRGs in treatments lasting 4-24 h. Flavopiridol has and immediate and long-term effect on the expression of several PRGs. In serum starved cells re-stimulated with serum, flavopiridol also inhibits the expression of these genes, but subsequently, JUNB, GADD45B and EGR1 are upregulated in the presence of flavopiridol.