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PQR530

CAS No. : 1927857-61-1

MCE 国际站：PQR530

产品活性：PQR530 是一种有效，ATP竞争性的，具有口服活性，可透过血脑屏障的，PI3K/mTORC1/2 双重抑制剂，对于 PI3Kα 和 mTOR (分别为 0.84 和 0.33 nM) 的 K_d 为亚摩尔。具有抗肿瘤活性。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K  |  mTOR

In Vitro: PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. PQR-530 inhibits all PI3K isoforms and mTOR complexes C1/2 potently and selectively. PQR-530 inhibits protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235/236) phosphorylation with IC₅₀ values of 0.07 µM in A2058 melanoma cells. PQR-530 shows inhibitory activity against the growth of 44 cancer cell lines with mean GI₅₀ of 426 nM.

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