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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-PQR309
PQR309

Chemical Structure : PQR309

CAS No.: 1225037-39-7

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PQR309 (Bimiralisib;PQR-309;PQR 309)

货号: PC-43268Not For Human Use, Lab Use Only.

PQR309 (Bimiralisib) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50 of 33, 451, 661, 708 and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2280 In stock
50 mg ￥3880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PQR309 (Bimiralisib) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50 of 33, 451, 661, 708 and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.
PQR309 (Bimiralisib) also shows potent activity against PI3Kα E542K/E545K/H2047R mutants with IC50 of 63/136/36 nM, shows no significant activity for VPS34 and DNA-PK (IC50>8,000 nM).
PQR309 (Bimiralisib) inhibits cellular phosphorylation of PKB/Akt on Ser473 and ribosomal S6 on Ser235/236 in A2058 melanoma cells with IC50 of 139 and 205 nM, SKOV3 cell growth IC50 is 237 nM.
PQR309 (Bimiralisib) demonstrates efficiency in inhibiting proliferation in tumor cell lines and rat xenograft models.

物理化学性质&存储条件

分子量 411.3816
分子式 C17H20F3N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Pyridinamine, 5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-

参考文献

1. Beaufils F, et al. J Med Chem. 2017 Sep 14;60(17):7524-7538.

2. Tarantelli C, et al. Clin Cancer Res. 2018 Jan 1;24(1):120-129.

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