pi3kα

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.

PI3Kα-IN-9 is an orally available, selective and potent PI3Kα inhibitor with antiproliferative activity, inhibits PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, induces apoptosis, and can be used in the study of cancer.

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

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

Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

BGT226 (NVP-BGT226) is a novel dual PI3K/mTOR inhibitor, targeting PI3K α, β, and γ with IC50 values of 4 nM, 63 nM, and 38 nM, respectively.

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

mTOR inhibitor 9c is a selective mTOR inhibitor with IC50 of 0.7nM and 825nM for mTOR and PI3Kα, respectively.

mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.

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.

CNX-1351 is a potent, isoform-selective, and targeted covalent inhibitor of PI3Kα.

AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.

NIBR-17 is a pan class I PI3K inhibitor. NIBR-17 inhibits PI3KKα, PI3KKβ, PI3KKγ, and PI3KKδ with IC50 of 1 nM, 9.2 nM, 9 nM, and 20 nM respectively.

HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).

ETP-46321 is an effective and orally bioavailable PI3Kα/PI3Kδ inhibitor (Ki: 2.3/14.2 nM).

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting over 10-1500 fold selectivity over other class I, II, and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM), and PI4KIIIB (IC50, 300.2 nM). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K and HDAC, with IC50 values of 8.1 nM and 1.4 nM, respectively.

PI3K-IN-6 is an oral active and highly selective inhibitor of phosphoinositide 3-kinase (PI3K) β/δ(IC50 values of 7.8 nM/5.3 nM , respectively).

PI3K/mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16.1, and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively. PI3K/mTOR Inhibitor-2 demonstrates antitumor activity.