pi3kα/mtor in 1

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.

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).

PI3K/mTOR ligand-1 is a ligand utilized for the PROTAC target protein (PI3K/mTOR). It is used in the synthesis of GP262.

PI3K/mTOR-IN-17 is a dual inhibitor that targets both PI3K and mTOR, with IC50 values of 1.21 μM and 0.21 μM, respectively. It induces apoptosis mediated by caspases and arrests cell growth in the G1 phase. The compound elevates the levels of caspases-3, 7, 8, and 9, enhances p53 expression, and increases the Bax/Bcl-2 ratio. By inhibiting the PI3K/mTOR signaling pathway, PI3K/mTOR-IN-17 is applicable in cancer research, including studies on non-small cell lung cancer (NSCLC).

PI3K/mTOR-IN-18 (Compound 12) is a highly selective dual inhibitor of PI3K/mTOR. It exerts antitumor effects through competitive binding to PI3Kα (Ki=0.130 nM) and mTOR (Ki=0.111 nM). By blocking the PI3K/AKT/mTOR pathway, PI3K/mTOR-IN-18 inhibits tumor cell proliferation (IC50=144 nM) and holds potential for research in solid tumors such as breast cancer and non-small cell lung cancer.

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

DHW-221 is an orally active dual PI3K/mTOR inhibitor demonstrating potent inhibition at nanomolar levels across all four Class I PI3K isoforms and mTOR (PI3Kα, IC50= 0.50 nM; PI3Kβ, IC50= 1.9 nM; PI3Kγ, IC50= 1.8 nM; PI3Kδ, IC50= 0.74 nM; mTOR, IC50= 3.9 nM). By blocking the PI3K/Akt/mTOR pathway, DHW-221 induces mitochondrial apoptosis and paraptosis (through endoplasmic reticulum stress and MAPK signaling) and causes cell cycle arrest, thereby inhibiting cell migration, invasion, and angiogenesis to exert its antitumor effects. It suppresses tumor growth in A549/Taxol and HCC827 mouse models and is applicable in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer[1][2][3].

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. It has IC50 values of 0.68, 1.02, 1.03, 8.03, and 15 nM for PI3Kα/β/γ/δ and mTOR, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines such as HCT-116 (IC50= 0.38 μM) and HT-29 (IC50= 1.70 μM). This compound is applicable in colorectal cancer (CRC) research.

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.

PI3Ka-IN-5 is a potent PI3Kα/mTOR inhibitor, with an IC 50 of 0.7 nM and 3.3 nM, respectively. PI3Ka-IN-5 can be used for the research of colorectal cancer .

PI3Kα-IN-1 is an inhibitor specifically targeting PI3Kα with an IC50 of less than 0.5 nM, and it also inhibits mTOR with an IC50 of 104 nM [1].