pik3ca

RLY-2608 is a selective mutant PI3Kα inhibitor that inhibits tumor growth in a PIK3CA mutant xenograft model.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8 12 65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

mTOR inhibitor 9b is an enzyme inhibitor of protein kinase mTOR he phosphatidylinositol 3-kinase PIK3CA with IC50s of 0.76 nm and 1.262 µM, respectively.mTOR inhibitor 9b possesses anticancer activity and can be used to study leukemia, skin, breast, lung and colon cancers.

mTOR inhibitor 9a inhibited the growth of human LNCap cells with an ic50 of 80 nm. 1-methyl-3 -{4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl}urea may have antitumor activity.

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

MK-2206 is an orally active, highly selective, metabotropic Akt inhibitor that targets Akt1 [IC50: 8 nM], Akt2 [IC50: 12 nM], and Akt3 [IC50: 65 nM]. Many breast cancer cell lines, PIK3CA mutants, and PTEN-losing cell lines are sensitive to MK-2206, which exhibits anti-cancer effects.

Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.

MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1].

MK-2206 free base is a potent, selective, and orally administered allosteric Akt inhibitor with IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. It demonstrates sensitivity in various breast cancer cell lines, including those with PIK3CA mutations and PTEN loss, indicating its potential for anticancer activities [1] [2].

Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].

BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα β δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA.

WAY-299017 is a potent and selective UPPS inhibitor for the treatment of bacterial infections.

JW-7-25-1 is a potent multi-target inhibitor, acting on MELK, PIK3CA, mTOR, GSK3A and CDK7.

Halociline, a derivative of alkaloids that can be isolated from the marine fungus Penicillium griseofulvum, targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells. This action is potentially mediated by diverse pathways, including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant, and biofilm inhibitory activities [1] [2].