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。

Motesanib Diphosphate

CAS No. : 857876-30-3

MCE 站：Motesanib Diphosphate

产品活性：Motesanib Diphosphate (AMG 706 Diphosphate) 是一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂，IC₅₀ 值为 2 nM/3 nM/6 nM，与对 Kit 的选择性相似，是 PDGFR 和 Ret 的 10 倍多。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：c-Kit  |  VEGFR

In Vitro: Motesanib Diphosphate (AMG 706 Diphosphate) has broad activity against the human VEGFR family, and displays over 1000-fold selectivity against EGFR, Src, and p38 kinase.Motesanib Diphosphate (AMG 706 Diphosphate) significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC₅₀ of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC₅₀ of >3,000 nM. Motesanib Diphosphate (AMG 706 Diphosphate) also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC₅₀ of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells. Although displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate (AMG 706 Diphosphate) treatment significantly sensitizes the cells to fractionated radiation.

In Vivo: Motesanib Diphosphate (AMG 706 Diphosphate) (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED₅₀ of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib Diphosphate (AMG 706 Diphosphate) induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib Diphosphate (AMG 706 Diphosphate) in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models. Motesanib Diphosphate (AMG 706 Diphosphate) treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Bevacizumab  |  Sunitinib  |  Imatinib  |  Semaxinib  |  SU 5402  |  PD173074  |  5Z-7-Oxozeaenol  |  Cediranib  |  SAR131675  |  Gandotinib  |  GW806742X  |  Tanshi IIA  |  PF-03814735  |  Vatalanib dihydrochloride  |  CP-547632  |  AST 487  |  Tyrphostin A9  |  Ki20227  |  Motesanib  |  SU14813  |  Ramucirumab  |  SU1498  |  MAZ51  |  PP121  |  ISCK03  |  Ki8751

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。