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Cat. No. Product Name CAS No. Information
PC-35326

Ch-319

Ch-319 (Ch319) is a triphenyltin (IV) carboxylate derivative that modulates AKT/FOXO3a signaling and inhibits progression of prostate cancer; reduces viability and induces cell cycle arrest associated with downregulation of PI3K and dephosphorylation of AKT and PRAS40 in PTEN-null PC3M and DU145 PCa cells at 250-500 nM; decreases tumor weights, reduces expression of androgen receptor, decreases phosphorylation of AKT and PRAS40 and increases FOXO3a in mice.
PC-63553

TAS-117 hydrochloride

TAS-117 is a potent, selective, allosteric inhibitor of Akt with IC50 of 4.8/1.6/44 for Akt1/2/3, respectively; displays no or only minimal inhibitory activities against other protein and lipid kinases, including PI3K, PDK1, and mTOR at 1 uM; inhibits Akt kinase activity but not p-Akt; induces significant growth inhibition, associated with downregulation of p-Akt, selectively in MM cell lines with high baseline p-Akt; significantly inhibits human MM cell growth in murine xenograft models, orally active.

Solid Tumors

Phase 2 Clinical

PC-63552

TAS-117

1402602-94-1 TAS-117 is a potent, selective, allosteric inhibitor of Akt with IC50 of 4.8/1.6/44 for Akt1/2/3, respectively; displays no or only minimal inhibitory activities against other protein and lipid kinases, including PI3K, PDK1, and mTOR at 1 uM; inhibits Akt kinase activity but not p-Akt; induces significant growth inhibition, associated with downregulation of p-Akt, selectively in MM cell lines with high baseline p-Akt; significantly inhibits human MM cell growth in murine xenograft models, orally active.

Solid Tumors

Phase 2 Clinical

PC-43440

CCT128930

885499-61-6 CCT128930 is a potent, selective, ATP-competitive AKT inhibitor with IC50 of 6 nM (AKT2), 28-fold selectivity over the closely related PKA; also exhibits 20-fold selectivity over p70S6K (IC50=120 nM); shows growth inhibition for U87MG human glioblastoma cells (IC50=6.3 uM), for LNCaP human prostate cancer cells (IC50=0.35 uM), and for PC3 human prostate cancer cells (IC50=1.9 uM) consistent with AKT pathway blockade; blocks the phosphorylation of several downstream AKT biomarkers in U87MG tumor xenografts, indicating AKT inhibition in vivo; demonstrates antitumor activity in U87MG and HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts.
PC-43434

A-674563 hydrochloride

A-674563 is a potent, selective and orally available AKT inhibitor with Ki of 11 nM (Akt1); increases the efficacy of paclitaxel in a PC-3 xenograft model; enhances the transcription of several chondrocyte marker genes, including Col2a1, Acan and Col11a2, in mouse primary chondrocytes by inhibiting Sox9 degradation through the ubiquitin-proteasome pathway; also suppresses FLT3-ITD positive AML both in vitro and in vivo.
PC-43433

A-674563

552325-73-2 A-674563 is a potent, selective and orally available AKT inhibitor with Ki of 11 nM (Akt1); increases the efficacy of paclitaxel in a PC-3 xenograft model; enhances the transcription of several chondrocyte marker genes, including Col2a1, Acan and Col11a2, in mouse primary chondrocytes by inhibiting Sox9 degradation through the ubiquitin-proteasome pathway; also suppresses FLT3-ITD positive AML both in vitro and in vivo.
PC-42878

PHT-427

1191951-57-1 PHT-427 is a small-molecule Akt inhibitor that binds selectively to the PH domain of AKT with Ki of 2.4 uM, inhibits phospho-Ser473-AKT in Panc-1 cells with IC50 of 6.3 uM; decreases AKT activation and causes apoptosis at low micromolar concentrations in Panc-1 and MiaPaCa-2 pancreatic cancer cell lines; inhibits AKT and its downstream targets in cells, exhibits good antitumor activity in pancreatic cancer cell xenografts in immunocompromised mice.

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