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。

SHP099

CAS No. : 1801747-42-1

MCE 国际站：SHP099

产品活性：SHP099是有效，选择性，有口服活性的 SHP2 抑制剂，IC₅₀ 值为70 nM。

研究领域：Protein Tyrosine Kinase/RTK  |  Metabolic Enzyme/Protease

作用靶点：SHP2  |  Phosphatase

In Vitro: The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC₅₀ of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells.

In Vivo: After a single dose of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Metabolism/Protease Compound Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Orally Active Compound Library  |  Phosphatase Inhibitor Library  |  Human Metabolite Library  |  Metabolic Enzyme Compound Library  |  Highly Selective Inhibitors Library  |  Multi-Target Compound Library  |  Bioactive Compound Library Max  |  Tacrolimus  |  β-Glycerophosphate disodium salt pentahydrate  |  Calyculin A  |  Okadaic acid  |  Sodium orthovanadate  |  Ebselen  |  Salubrinal  |  Ellagic acid  |  Batoprotafib  |  L-Ascorbic acid 2-phosphate trisodium  |  Osunprotafib  |  Suramin sodium salt  |  RMC-4550  |  TPI-1  |  Sodium metatungstate  |  GSK 2830371  |  DT-061  |  D-erythro-Sphingosine  |  SF1670  |  Vociprotafib  |  Idoxuridine  |  LB-100  |  NSC 663284  |  SHP099 monohydrochloride  |  BCI  |  BTdCPU  |  MSI-1436 lactate

热门产品线：重组蛋白  |  药物筛选  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

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域；
•   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。