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.

(S)-PI3Kα-IN-4, a potent inhibitor of PI3Kα with an IC50 of 2.3 nM, demonstrates 38.3-, 4.25-, and 4.93-fold selectivity over PI3Kβ, PI3Kδ, and PI3Kγ, respectively, and is suitable for cancer research[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1].

PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1].

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.

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/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.

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM).

PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.

PI3K-IN-38 is an orally available and potent PI3K inhibitor with an IC50 value of 0.541 µM for PI3K-α. PI3K-IN-38 exhibits anticancer and anti-inflammatory activity and inhibits tumor growth in vivo.

PI3Kα Inhibitor 7 is a useful organic compound for research related to life sciences. The catalog number is T9312 and the CAS number is 1239978-63-2.

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.

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.

STX-478 is an orally active and selective PI3Kα inhibitor that penetrates the blood-brain barrier and has anticancer activity to inhibit tumor growth.STX-478 is indicated for the study of breast cancer and other cancers.

RLY-2608 is a small molecule inhibitor, a selective allosteric PI3Kα inhibitor with high selectivity for PIK3CA mutations. This compound effectively inhibits tumor growth in PIK3CA-mutant xenograft models and is primarily used for research on PIK3CA-driven cancers.

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 9f is a selective mTOR inhibitor with IC50 of 1.25nM and 82nM for mTOR and PI3Kα, respectively.

mTOR inhibitor 9e is a selective mTOR inhibitor with IC50 of 0.68nM and 1359nM for mTOR and PI3Kα, respectively.

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