pi-3kα-in-4

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

PI3K-IN-46 is a specific inhibitor of PI3Kγ.

PI3K-IN-47 (Compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (PI3K) family, with IC50 values of 0.44 nM for PI3Kα, and 7.18 nM, 13.92 nM, and 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ respectively. It induces G1 phase cell cycle arrest and exhibits anti-neoplastic properties by restraining colony formation and cell migration. Additionally, PI3K-IN-47 has demonstrated the ability to suppress tumor growth in HGC-27 xenograft mouse models [1].

PI3K-IN-41 (compound 2), a photocaged PI3K inhibitor (IC50=18.92 nM) with anticancer properties, demonstrates potent PI3K inhibition following UV light irradiation and has been shown to enhance antitumor effects [1]. This compound has potential for use in precisely controlled cancer therapeutics.

PI3K-IN-48, a PI3K inhibitor, exhibits an IC50 of 1.55 ± 0.18 μM in A549 cells, demonstrating its potency in this context. It induces G0/G1 phase arrest and cell apoptosis, while also down-regulating the expression of p-PI3K and p-Akt. This compound is relevant for research into the treatment of human lung cancers [1].

PI3K-IN-49 is a powerful inhibitor of PI3K, demonstrating antiproliferative effects on Avg T-47D and Avg SKBR3 cells (WO2023239710A1; example 29) [1].

(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].