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。

UM-164

CAS No. : 903564-48-7

MCE 站：UM-164

产品活性：UM-164 (DAS-DFGO-II) 是一种高效的 c-Src 抑制剂，K_d 为 2.7 nM。UM-164 还高效抑制 p38α 和 p38β 活性。

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

作用靶点：Src  |  p38 MAPK  |  Autophagy

In Vitro: In biochemical assays, UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 K_d=2.7 nM, Dasatinib K_d=0.7 nM). To confirm that UM-164 is capable of inhibiting the activation of c-Src in vitro, the effect of UM-164 is examined on the c-Src autophosphorylation in two TNBC cell lines (MDA-MB 231 ａnd SUM 149). Inhibition of c-Src autophosphorylation is detected in a concentration- ａnd a time-dependent manner. At 120 minutes, complete abrogation of c-Src autophosphorylation is observed at 50 nM, demonstrating that UM-164 is a potent c-Src inhibitor in vitro. Flow cytometry experiments demonstrate that UM-164 treatment of MDA-MB 231 ａnd SUM 149 increased the proportion of G₀-G₁ cells by 25% ａnd 28%, respectively, ａnd concurrently decreased the fraction of S cells by 16% ａnd 19%, respectively.

In Vivo: A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 ａnd SUM 149 cell lines. Once the tumors become palpable, the mice are randomized into control ａnd treatment groups. Mice are injected intraperitoneally with either drug (10 ａnd 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164, there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg ａnd 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 ａnd P<0.004, respectively).

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Pyroptosis Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Antidepressant Compound Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  Tirbanibulin dihydrochloride  |  HIV-IN-6  |  Bisabolangelone  |  4-Hydroxylonchocarpin  |  Bafetinib  |  Multi-kinase-IN-2  |  PP2  |  TLR4/NF-κB/MAPK-IN-1  |  Cannabisin D  |  PP58  |  PLK1/p38γ-IN-1  |  Broussonin E  |  L-threo-Sphingosine  |  SB 242235  |  ENMD-2076 Tartrate  |  Hydrangenol  |  Lck-IN-1  |  EGF-R (661-681) T669 Peptide  |  p38 Kinase inhibitor 5  |  TA-01  |  Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH  |  AMG-548 hydrochloride  |  Ponatinib hydrochloride  |  JX401  |  Ganoderterpene A  |  VX-702  |  Org 48762-0  |  TL02-59 dihydrochloride  |  Esculin  |  R1487 Hydrochloride

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*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。