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PQR-530
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PQR-530图片
CAS NO:1927857-61-1
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
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。
Cas No.1927857-61-1
Canonical SMILESFC(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4[C@H](COCC4)C)=N2)F
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
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).