BAY 1082439

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY 1082439 是一种有效、高选择性、口服的 PI3Kα/β 抑制剂，选择性抑制两种 PI3Kα。

BAY 1082439 is a potent, highly selective, orally available PI3Kα/β inhibitor, selectively inhibits both PI3Kα, including mutated forms of PIK3CA, and PI3Kβ in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K-expressing and/or PTEN-driven tumor cells.Solid Tumors Phase 1 Clinical(In Vitro):BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase.BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.(In Vivo):BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression.

BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase.BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells. TCell Viability Assay Cell Line:PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines) Concentration:0.1, 0.33, 1, 3.3, 10 μM Incubation Time:72 hours Result:Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis.

BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression. Animal Model: Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)Dosage:75 mg/kg Administration:P.o.; daily for 4 weeks Result:Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.

BAY 10-82439 | BAY1082439

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

Solid Tumors

1375469-38-7

494.228

C25H30N6O5

>98% (HPLC)

In Vitro:?DMSO : 5 mg/mL (10.11 mMult)

C1=CC(OC[C@@H](O)CN2CCOCC2)=C(OC)C2N=C(NC(=O)C3=CC=CN=C3C)N3CCN=C3C1=2

(S)-N-(8-(2-hydroxy-3-morpholinopropoxy)-7-methoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)-2-methylnicotinamide

(-20℃)

With Ice Pack

≥ 2 years