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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-PF-04691502
PF-04691502

Chemical Structure : PF-04691502

CAS No.: 1013101-36-4

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PF-04691502 (PF04691502)

货号: PC-23844Not For Human Use, Lab Use Only.

PF-04691502 is a potent, selective, ATP-competitive PI3K/mTOR dual inhibitor with Ki of 1.8/1.2 nM (human/mouse PI3Kα), 2.1/1.6/1.9 nM (PI3Kβ/δ/γ) and 16 nM (human mTOR).

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5 mg ￥580 In stock
10 mg ￥880 In stock
25 mg ￥1480 In stock
50 mg ￥2580 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

PF-04691502 is a potent, selective, ATP-competitive PI3K/mTOR dual inhibitor with Ki of 1.8/1.2 nM (human/mouse PI3Kα), 2.1/1.6/1.9 nM (PI3Kβ/δ/γ) and 16 nM (human mTOR).
PF-04691502 inhibits recombinant mouse PI3Kα in an ATP-competitive inhibitor.
PF-04691502 shows no significant inhibitory activity against > 80 protein kinases at 10 uM, including class III PI3K family member hVps34, PI3K downstream kinases AKT, PDK1, p70S6K, and MAPK family members such as MEK, ERK, p38, and JNK.
PF-04691502 potently inhibits AKT phosphorylation on S473 and T308 in cancer cell lines with IC50 values of 3.8 to 20 nmol/L and 7.5 to 47 nmol/L, respectively.
PF-04691502 induces cell cycle G1 arrest, concomitant with upregulation of p27 Kip1 and reduction of Rb.
PF-04691502 exhibits antitumor activity was observed in U87 (PTEN null), SKOV3 (PIK3CA mutation), and gefitinib- and erlotinib-resistant non–small cell lung carcinoma xenografts.

物理化学性质&存储条件

分子量 425.49
分子式 C22H27N5O4
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-Amino-8-(rel-(1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one

参考文献

1. Yuan J, et al. Mol Cancer Ther. 2011 Nov;10(11):2189-99.

2. Kinross KM, et al. Mol Cancer Ther. 2011 Aug;10(8):1440-9.

3. Cheng H, et al. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7.

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