pi3kα inhibitor 7

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.

PI3Kγ Inhibitor 7 (compound 2) is a potent, orally active agent that selectively inhibits PI3Kγ with an IC50 of 3.42 nM and demonstrates antitumor activity [1]. It also exhibits varying inhibitory effects on other PI3K isoforms, with IC50 values of 4768 nM for PI3Kα, 878.1 nM for PI3Kβ, and 355.2 nM for PI3Kδ.

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.

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor targeting PI3K and mTOR, with IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. It also inhibits mTORC1 and mTORC2.

WYE-687 is an ATP-competitive and selective inhibitor of mTOR with an IC50 of 7 nM; it blocks mTORC1 pS6K(T389) and mTORC2 P-AKT(S473) without affecting P-AKT(T308). Its selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

(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].

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

PI3Kα-IN-7 (Compound A12) is a potent inhibitor of PI3Kα and PI3Kβ, capable of reducing mitochondrial membrane potential in cancer cells and inducing apoptosis.

WYE-687 dihydrochloride is an ATP-competitive inhibitor of mTOR, demonstrating potent activity with an IC50 value of 7 nM. It effectively suppresses the activation of both mTORC1 and mTORC2. Additionally, WYE-687 exhibits inhibitory effects on PI3Kα and PI3Kγ, with IC50 values of 81 nM and 3.11 μM, respectively.

FD2056 is a potent, orally active PI3K inhibitor, with IC50 values of 0.30, 0.80, 1.10, and 0.42 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Additionally, it exhibits inhibitory effects on CDK2-CyclinA2 and CDK4-CyclinD3 with IC50s of 115.95 nM and 2782.15 nM. FD2056 effectively inhibits the proliferation of various breast cancer cell lines, such as MDA-MB-231, MDA-MB-468, and MCF-7, with IC50s of 1.06 μM, 0.04 μM, and 1.40 μM, respectively. The compound also promotes apoptosis in cancerous cells and has been shown to suppress tumor growth [1].

PI3Kα-IN-13 (Compound 18a), a PI3Kα inhibitor with an IC50 of 2.5 nM, effectively induces apoptosis and hampers the proliferation of various cancer cell lines, exhibiting IC50 values of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), and 9.85 μM (SW620). This compound also impedes tumor cell colony formation, migration, and invasion [1].

PI3Kα-IN-15 is a powerful inhibitor of PI3Kα, exhibiting an IC₅₀ of 0.15 μM. It shows promising anti-proliferative effects, inhibiting the growth of SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 cell lines with respective IC₅₀ values of 26.6 μM, 7.9 μM, 32.1 μM, 17.7 μM, and 9.4 μM. This compound is useful for cancer research [1].