BAY1082439 是一种具有口服活性的，选择性PI3Kα/β/δ抑制剂。BAY1082439 也能抑制 PIK3CA 的突变形式，BAY1082439 对抑制Pten丢失的前列腺癌的生长有很强的作用。
| 生物活性 | BAY1082439 is an orally bioavailable, selectivePI3Kα/β/δinhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibitingPten-null prostatecancergrowth[1][2]. |
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体外研究
(In Vitro) | BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase[1].
BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells[2].
Cell Viability Assay[2] | 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. |
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体内研究
(In Vivo) | BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventingPten-null prostate cancer progression[2].
| Animal Model: | Pten conditional knockout mouse model (Pb-Cre+;PtenL/L, CP model)[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(10.11 mM;ultrasonic and adjust pH to 5 with HCl) 配制储备液 | 1 mM | 2.0221 mL | 10.1104 mL | 20.2208 mL | | 5 mM | 0.4044 mL | 2.0221 mL | 4.0442 mL | | 10 mM | 0.2022 mL | 1.0110 mL | 2.0221 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
