p110α-h1047r

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

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.

Buparlisib Hydrochloride (BKM120 HCl) is a specific and orally bioavailable pan-class I PI3K inhibitor that competitively inhibits PI3K/AKT kinase at the nanomolar level and suppresses cancer cell growth, making it suitable for studying breast cancer, glioblastoma, and solid tumours.

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.

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

Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).

Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.

Pictilisib (GDC-0941) (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ).

(S)-Phe-A110/B319 is a selective binder with a 20-fold higher affinity for the H1047R mutant of the p110α subunit within the p110α/p85α PI3K complex.

PI3Kα-IN-29 is an efficacious, orally bioavailable, and selective PI3Kα inhibitor with an IC50 value of 2.5 nM. It demonstrates over 400-fold selectivity against PI3Kβ/δ/γ/mTOR. This compound selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses the PI3K/AKT/mTOR signaling pathway, induces G1 phase arrest, and inhibits cell migration. Additionally, it impedes tumor growth in T47 mouse models and is applicable for breast cancer research.

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

(R)-Phe-A110/B319 is a hapten and a selective binder for tumor-associated antigens. It exhibits a 20-fold higher affinity for the H1047R mutant of p110α within the p110α/p85α PI3K complex. This compound is applicable in studies on the activation of conditional chimeric antigen receptor T (CAR-T) cells and tumor targeting.