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。

GSK1904529A

CAS No. : 1089283-49-7

MCE 站：GSK1904529A

产品活性：GSK1904529A 是一种有效的，选择性的，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体 (IGF-1R) 和胰岛素受体 (IR) 抑制剂，IC₅₀ 值分别为 27 和 25 nM。GSK1904529A 在其他 45 种丝氨酸/苏氨酸和酪氨酸激酶中显示出较弱的活性 (IC₅₀>1 μM)。GSK1904529A 具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：IGF-1R  |  Insulin Receptor  |  Apoptosis

In Vitro: GSK1904529A displays high affinities for IGF-1R and IR, with K_is of 1.6 and 1.3 nM, respectively.
GSK1904529A (72 h) inhibits tumor cells proliferation with IC₅₀s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive.
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle.
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC₅₀s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively.
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells.

In Vivo: GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice.
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice.
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Diabetes Related Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Insulin (human)  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rotenone  |  Etomoxir  |  Stattic  |  Docetaxel

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。