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。

Perifosine

CAS No. : 157716-52-4

MCE 国际站：Perifosine

产品活性：Perifosine是一种有口服活性的 Akt 抑制剂，抑制不同肿瘤细胞系增殖的 IC₅₀ 值为0.6-8.9 μM。

研究领域：PI3K/Akt/mTOR  |  Autophagy  |  Apoptosis

作用靶点：Akt  |  Autophagy  |  Apoptosis

In Vitro: The IC₅₀ for growth of Ntv-a/LacZ cell lines is determined by MTT assay. When the cells are cultured for 48 hours in 10% FCS-supplemented media, the IC₅₀ for cells with constitutively active PDGF, Ras, or Akt signaling is similar and found to be ~45 μM.Perifosine, a oral-bioavailable alkylphospholipid (ALK), on the cell cycle kinetics of immortalized keratinocytes (HaCaT) as well as head and neck squamous carcinoma cells. Proliferation is assessed by the incorporation of [³H]thymidine into cellular DNA. Exposure to Perifosine (0.1-30 μM) for 24 h results in a dose-dependent inhibition of [³H]thymidine uptake in all cell lines tested. The IC₅₀s for growth are between 0.6 and 8.9 μM, reaching IC₈₀s of ~10 μM. Perifosine blocks cell cycle progression of head and neck squamous carcinoma cells at G₁-S and G₂-M by inducing p21^WAF1, irrespective of p53 function, and may be exploited clinically because the majority of human malignancies harbor p53 mutations. Perifosine (20 μM) induces both G₁-S and G₂-M cell cycle arrest, together with p21^WAF1 expression in both p53 wild-type and p53^-/- clones.

In Vivo: Mice are identified with tumors by bioluminescence imaging and either treated them with 100 mg/kg Temozolomide, or 30 mg/kg Perifosine, or a combination with 100 mg/kg Temozolomide and 30 mg/kg Perifosine (Temozolomide+Perifosine) for 3 to 5 days. The mice are sacrificed and tumors analyzed histologically for cell proliferation by Ki-67 immunostaining. Ki-67 staining index is significantly reduced in mice treated with either Temozolomide (Ki-67 staining index=5.5±1.2%, n=4, P=0.0019) or Perifosine (Ki-67 staining index=3.2±1.1%, n=3, P=0.001) compared with Control, demonstrating the inhibitory effect on proliferation. Most importantly, the tumors treated with Temozolomide+Perifosine have the lowest Ki-67 staining index (1.7±1.2%, n=3, P=0.0005). The additional treatment with Perifosine results in a significantly lower proliferation rate than Temozolomide alone (P=0.0087). Perifosine markedly decreases p-Akt from 10 min to 24 hours and subsequently, moderately decreased p-S6 from 1h to 24 h after injection.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  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  |  Differentiation Inducing Compound Library  |  Lipid Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Glutamine Metabolism Compound Library  |  FDA Approved & Pharmacopeial Drug 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  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Glucose Metabolism Compound Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Anti-Colorectal Cancer Compound Library   |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Cancer Stem Cells Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  SY-5609  |  BRD4 Inhibitor-18  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Anticancer agent 120  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  Thailanstatin D  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  CR-1-31-B  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  LM22B-10  |  AZA1  |  Antitumor agent-96  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，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；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。