PF-04691502,1013101-36-4

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PF-04691502

CAS No. : 1013101-36-4

MCE 国际站：PF-04691502

产品活性：PF-04691502是有效和选择性的 PI3K 和 mTOR 的抑制剂。 PF-04691502与人PI3Kα，β，δ，γ和mTOR结合的 K_i 分别为1.8，2.1，1.6，1.9和16 nM。

研究领域：PI3K/Akt/mTOR  |  Autophagy

作用靶点：PI3K  |  mTOR  |  Autophagy

In Vitro: PF-04691502 inhibits recombinant mouse PI3Kα in an ATP-competitive inhibitor. PF-04691502 potently inhibits AKT phosphorylation on S473 and T308 in all the 3 cancer cell lines with IC₅₀ values of 3.8 to 20 nM and 7.5 to 47 nM, respectively. Using a 96-well plate-based P-S6RP(S235/236) ELISA assay, PF-04691502 potently inhibits mTORC1 activity with an IC₅₀ of 32 nM. PF-04691502 inhibits cell proliferation of BT20, SKOV3, and U87MG with IC₅₀ values of 313, 188, and 179 nM, respectively. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 reduces phosphorylation of AKT T308 and AKT S473 (IC₅₀ of 7.5-47 nM and 3.8-20 nM, respectively) and inhibits cell proliferation (IC₅₀ of 179-313 nM). PF-04691502 inhibits mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC₅₀ of 32 nM and inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP.

In Vivo: Nude mice bearing U87MG tumors are administered orally once a day with PF-04691502 at 0.5, 1, 5, and 10 mg/kg (maximum tolerated dose, MTD). Treatment with 10 mg/kg results in a significant reduction of P-AKT(S473) levels at 1 hour postdosing, and persistent inhibition is observed for 8 hours. P-AKT(S473) recovers to above baseline 24 hours after 10 mg/kg treatment. For P-S6RP(S235/236), a similar inhibition time course is observed, but after 24 hours of treatment, P-S6RP levels remain lower than vehicle tumors. Modulation of the AKT downstream effector, P-PRAS40(T246), and mTOR downstream effector, P-4EBP1(T37/46), is observed. The PF-04691502-treated tumors are also evaluated by immunohistochemistry for levels of P-AKT(S473), total AKT, P-S6RP, and total S6RP. Phosphorylation of AKT and S6RP are significantly reduced at 4 hours after a single dose of PF-04691502 at 10 mg/kg. Dose-dependent tumor growth inhibition (TGI) is obtained in the U87MG xenograft model and approximately 73% TGI is observed at the MTD dose of 10 mg/kg.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Antioxidant Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Angiogenesis-Related Compound Library  |  Glucose Metabolism Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Rapamycin  |  3-Methyladenine  |  LY294002  |  Alpelisib  |  Quercetin  |  Everolimus  |  MHY1485  |  Wortmannin  |  Torin 1  |  740 Y-P  |  AZD-8055  |  Idelalisib  |  Buparlisib  |  Inavolisib  |  Dactolisib  |  Sapanisertib  |  Eganelisib  |  Pictilisib  |  Copanlisib  |  SAR405  |  JR-AB2-011  |  3BDO  |  Duvelisib  |  Salidroside  |  Torin 2  |  Temsirolimus  |  Recilisib  |  YM-201636  |  L-Leucine  |  Torkinib

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物  |  寡核苷酸

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。