PQR-530是一种有效，可口服，可透过血脑屏障的，广谱的PI3K/mTORC1/2双重抑制剂，具有抗肿瘤活性。
货号:ajcx13044
CAS:1927857-61-1
分子式:C18H23F2N7O2
分子量：407.42
溶解度:DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.33 mg/ml,DMSO: 10 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.

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[1].

[1]. Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor. Cancer Res 2017;77(13 Suppl).