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。

KG5

CAS No. : 877874-85-6

MCE 站：KG5

产品活性：KG5 是一种具有口服活性的双重 PDGFRβ 和 B-Raf 变构抑制剂。KG5 还抑制 Flt3，KIT 和 c-Raf，并具有抗癌，抗血管生成活性。

研究领域：MAPK/ERK Pathway  |  Protein Tyrosine Kinase/RTK

作用靶点：Raf  |  PDGFR  |  FLT3  |  c-Kit

In Vitro: KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) ａnd endothelial cells viability with EC₅₀ values of 0.59 μM ａnd 0.54 μM, respectively.
Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259.
KG5 (Compound 6) inhibits only PDGFRα ａnd β with K_ds of 300 ａnd 520 nM, respectively, ａnd Flt3 ａnd KIT at 52 ａnd 170 nM, respectively.
KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK ａnd ERK in endothelial cells stimulated with bFGF or VEGF.

In Vivo: KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model.
KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose ａnd formulation of KG5 used indicated a C_max of 3.6 μg/mL, T_1/2 of 11.5 h, ａnd an area under the concentration time curve (AUC_0-12h) of 14.7 μg•h/mL.
KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis.

相关产品：Sunitinib  |  Imatinib  |  Doramapimod  |  SU 5402  |  Cediranib  |  AT9283  |  GW 5074  |  Gandotinib  |  Ro 5126766  |  KW-2449  |  Lestaurtinib  |  AZ 628  |  GDC-0879  |  ZM 336372  |  CG-806  |  AST 487  |  Ki20227  |  Motesanib  |  SU14813  |  PP121  |  Sennoside B  |  ISCK03  |  PP58  |  AG 1295  |  Agerafenib  |  JNJ-47117096 hydrochloride  |  Methylnissolin

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。