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

Chemical Structure : Izorlisib

CAS No.: 1007207-67-1

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Izorlisib (MEN1611, CH5132799)

货号: PC-73424Not For Human Use, Lab Use Only.

Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.

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5 mg ￥1280 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4880 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

Izorlisib (MEN1611, CH5132799) is a potent, selective, orally available class I PI3K inhibitor with IC50 of 14/120/400/36 nM against PI3Kα/β/δ/γ, respectively.
Izorlisib (CH5132799) shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 >10 μM) against 26 protein kinases.
Izorlisib (CH5132799) exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα.
Izorlisib (CH5132799) effectively suppresses phosphorylation of Akt PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1 in breast cnacer KPL-4 cells.
Izorlisib (CH5132799) shows potent in vivo antitumor activity in several different xenograft models with PIK3CA mutations.

物理化学性质&存储条件

分子量 377.423
分子式 C15H19N7O3S
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

5-[7-(methanesulfonyl)-2-(morpholin-4-yl)-6,7-dihydro5H-pyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amine

参考文献

1. Ohwada J, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72.

2. Tanaka H, et al. Clin Cancer Res. 2011 May 15;17(10):3272-81.

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