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Cat. No. Product Name CAS No. Information
PC-36126

Borussertib

1800070-77-2 Borussertib is a potent, first-in-class, covalent-allosteric AKT inhibitor; specifically binds to two non-catalytic cysteines in AKT at 120 positions 296 and 310; exhibits pronounced sensitivity to breast cancer cell line ZR-75-1 with EC50 of 5 nM, 7- to 12-fold higher potency compared to reversible allosteric inhibitor miransertib and MK-2206; demonstrated strong antiproliferative activity in cancer cell lines harboring genetic alterations within the PTEN, PI3K, and RAS signaling pathways,b displayed antitumor activity in combination with the MEK inhibitor trametinib in patient-derived xenograft models of mutant KRAS pancreatic and colon cancer.
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.

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