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BAY1082439 是一种具有口服活性的,选择性 PI3Kα/β/δ抑制剂。它也能抑制 PIK3CA 的突变形式,它对抑制 Pten 丢失的前列腺癌的生长有很强的作用。
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BAY1082439 是一种具有口服活性的,选择性 PI3Kα/β/δ抑制剂。它也能抑制 PIK3CA 的突变形式,它对抑制 Pten 丢失的前列腺癌的生长有很强的作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 315 | 现货 | |
2 mg | ¥ 453 | 现货 | |
5 mg | ¥ 728 | 现货 | |
10 mg | ¥ 1,230 | 现货 | |
25 mg | ¥ 1,980 | 现货 | |
50 mg | ¥ 3,730 | 现货 | |
100 mg | ¥ 5,380 | 现货 |
产品描述 | BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2]. Additionally, BAY1082439 is effective against mutated forms of PIK3CA. |
体外活性 | BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. 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]. 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[1]. |
体内活性 | BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression[2]. |
别名 | N-[8-[[(2R)-2-羟基-3-(吗啉-4-基)丙基]氧基]-7-甲氧基-2,3-二氢咪唑并[1,2-C]喹唑啉-5-基]-2-甲基吡啶-3-甲酰胺 |
分子量 | 494.54 |
分子式 | C25H30N6O5 |
CAS No. | 1375469-38-7 |
Smiles | COc1c(OC[C@H](O)CN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cccnc3C)=Nc12 |
密度 | 1.43 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: Slightly soluble |
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