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A major introduction to RG7388!

RG7388(cas 1229705-06-9) is an oral, selective, small molecule MDM2 antagonist that inhibits binding of MDM2 to p53. RG7388 binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis.

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A major introduction to Autophinib!

Autophinib(cas 1644443-47-9) is a potent autophagy inhibitor, which can inhibit autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34 with IC50s of 90, 40 and 19 nM, respectively.

E 3810 is in stock now!

First-in-class dual VEGFR/FGFR tyrosine kinase inhibitor; E-3810 potently and selectively inhibited VEGFR1, -2, and -3 and FGFR-1 and -2 kinases in the nanomolar range; a potent antiangiogenic small molecule with a favorable pharmacokinetic profile and broad spectrum antitumor activity

A major introduction to BYL-719!

BYL719(cas 1217486-61-7) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, liitle or no effect on PI3Kβ/γ/δ. BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway.