13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:PF-04691502
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
| CAS | 1013101-36-4 |
| 別名 |
|
| 化學名 | 2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one |
| 分子式 | C22H27N5O4 |
| 分子量 | 425.48 |
| 溶解度 | ≥ 10.625mg/mL in DMSO with gentle warming |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
PF-04691502 is a potent and selective dual PI3K/mTOR (FRAP) inhibitor to phosphorylation of Akt T308 (IC50 = 7.5 nM) and Akt S473 (IC50 = 3.8 nM).[1]
PI3Ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.The functions of PI3Ks most relate to the ability of class I PI3K to activate protein kinase B (PKB, aka Akt) as in the PI3K/AKT/mTOR pathway which is an intracellular signaling pathway directly related to cellular quiescence, proliferation, cancer, and longevity. There are many valuable anti-cancer drug treatment targets within this pathway. And also the p110δ and p110γ isoforms regulate different aspects of immune responses. [2]
PF-04691502 is a potential medical drug that functions by inhibiting class I PI3K and mTOR in the PI3K/AKT/mTOR pathway through fluorescence polarization kinase assay, cell,mice and other animal trials, and therefore, through inhibition, results in tumour suppression.[3,4] Short-term exposure to PF-04691502 predominantly inhibits PI3K, whereas mTOR inhibition persists for 24 to 48 hours. PF-04691502 induces cell cycle G(1) arrest, concomitant with upregulation of p27 Kip1 and reduction of Rb. [5] Antitumor activity of PF-04691502 is observed in U87 (PTEN null), SKOV3 (PIK3CA mutation), and gefitinib- and erlotinib-resistant non-small cell lung carcinoma xenografts. PF-04691502 inhibits tumor growth at 7 days by 72%. FDG-PET imaging revealed that PF-04691502 reduces glucose metabolism dramatically. Tissue biomarkers of PI3K/mTOR pathway activity, p-AKT (S473), and p-RPS6 (S240/244), are also dramatically inhibited following PF-04691502 treatment. [6]
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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