PQR-530

A dual inhibitor of PI3Kα and mTOR

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
250mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajcx13044
CAS: 1927857-61-1
别名:
分子式: C18H23F2N7O2
分子量: 407.42
纯度: >98%
溶解度: DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.33 mg/ml,DMSO: 10 mg/ml
储存: Store at -20°C
库存: 现货

Background

PQR530 is a dual inhibitor of PI3Kα and mammalian target of rapamycin (mTOR; IC₅₀s = 11.1 and 7.4 nM, respectively).¹ It inhibits phosphorylation of Akt and ribosomal S6 kinase in A2058 melanoma cells (IC₅₀s = 62.2 and 61.1 nM, respectively). PQR530 inhibits cell growth in a panel of 66 cancer cell lines (mean GI₅₀ = 0.43 ?M). In vivo, PQR530 (25 mg/kg) reduces tumor growth in an OVCAR-3 ovarian cancer mouse xenograft model. It decreases the number of seizures per week in a Tsc1^GFAP conditional knockout mouse model of epilepsy.²

1.Rageot, D., Bohnacker, T., Keles, E., et al.(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530, a potent, orally bioavailable and brain penetrable dual inhibitor of class I PI3K and mTOR kinaseJ. Med. Chem.62(13)6241-6261(2019) 2.Theilmann, W., Gericke, B., Schidlitzki, A., et al.Novel brain permeant mTORC1/2 inhibitors are as efficacious as rapamycin or everolimus in mouse models of acquired partial epilepsy and tuberous sclerosis complexNeuropharmacology180108297(2020)