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PQR-530 (PQR530) is a potent, BBB penetrant, dual pan-PI3K/mTOR inhibitor with Kd of 0.3/1/6/11/10 nM for mTOR/PIK3CA/PIK3CB/PIK3CD/PIK3CG, respectively; effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy.




Umbralisib (RP5264,TGR1202, TGR-1202) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM, 50-fold selectivity over PI3Kα/β and >10,000 fold over PI3Kγ; enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest, demonstrates highly synergistic effect with the proteasome inhibitor carfilzomib in lymphoma, leukemia, and myeloma cell lines and primary lymphoma and leukemia cells; synergistically disrupts the 4E-BP1-eIF4F-c-Myc axis with carfilzomib, also potently inhibits 60% of the activity of CK1ε at 1 uM.

Blood Cancer

Phase 3 Clinical




SF-1126 is a pan PI3K/BRD4 inhibitor, RGDS-conjugated LY294002 prodrug that exhibits increased solubility and binds to specific integrins; blocks expression levels of c-Myc in HCC cells, inhibits proliferation, cell cycle, apoptosis, PI3K/AKT/mTOR and Ras/Raf/MAPK pathway; shows significant antitumor activity in vivo.

Liver Cancer

Phase 1 Clinical




SN-32976 is a novel, potent and selective class I PI3K and mTOR inhibitor with IC50 of 15.1/461/110/134/194 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR, respectively; displays preferential activity for PI3Kα and spares PI3Kδ relative to the other inhibitors, and shows less off-target activity in a panel of 442 kinases; inhibits pAKT expression and cell proliferation at nM concentration, induces a greater extent and duration of pAKT inhibition in tumors than pictilisib, dactolisib and omipalisib in animal models.




Autophinib is a novel, potent autophagy inhibitor that inhibits autophagy induced by starvation (IC50=90 nM) or rapamycin (IC50=40 nM) by targeting the lipid kinase VPS34 (IC50=19 nM); inhibits LC3 lipidation to form LC3-II, also inhibits p62 degradation dose-dependently in starved MCF7-LC3 cells; an ATP-competitive inhibitor of VPS34 but not other lipid kinases, mTOR and TBK1.




GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=9.9); displays >1000 fold selectivity versus other PI3K isoforms; inhibits both IFNγ and IL-2 production in a concentration-dependent manner, with pIC50 values of 8.2 and 8.1, respectively, in a human lung parenchyma assay; shows activity in rat acute OVA model of Th2-driven lung inflammation (ED50=67ug/kg).


Phase 2 Clinical




NVP-BKM120 (BKM-120, Buparlisib) is a potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively; much less effectively inhibits the class III PI3K Vps34 and mTOR, and has no effect on PI4Kβ and several other kinases; prevents the growth of assorted cancer cell lines when used at 5 μM and inhibits tumor growth in vivo.

Blood Cancer

Phase 2 Clinical

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