MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務。

Fruquintinib

CAS No. : 1194506-26-7

產品活性：Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC₅₀s of 33, 0.35, and 35 nM, respectively.

研究領域：Protein Tyrosine Kinase/RTK

作用靶點：VEGFR

In Vitro: Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC₅₀s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC₅₀s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours.

In Vivo: Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4～98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg.

相關產品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  NMPA-Approved Drug Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Therapy Drug Library   |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  FDA-Approved Anticancer Drug Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  5α-Hydroxycostic acid  |  GW806742X hydrochloride  |  Sorafenib-d₄  |  BMS-690514  |  VEGFR-2-IN-6  |  PROTAC VEGFR-2 degrader-1  |  Multi-kinase-IN-2  |  Sorafenib Tosylate  |  K00546  |  c-Met-IN-11  |  VEGFR-2-IN-29  |  Threo-Chloramphenicol-d₆  |  Foretinib  |  ZM323881 hydrochloride  |  ODM-203  |  Taurocholic acid sodium  |  VEGFR-2/DHFR-IN-2  |  ENMD-2076 Tartrate  |  Albendazole  |  SU5408  |  R1530  |  AZD2932  |  Toceranib phosphate  |  EGFR-IN-57  |  Bevasiranib  |  Ponatinib hydrochloride  |  VEGFR-2-IN-28  |  Famitinib malate  |  AhR modulator-1  |  Hypothemycin

熱門產品線：重組蛋白  |  化合物庫  |  天然產物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領；
•   產品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產品，廣泛應用于新藥研發、生命科學等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學分析檢測分析，藥物篩選等專業技術服務；
•   設有專業的實驗中心和嚴格的質控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質檢報告，確保產品的高純度、高品質；
•   產品的生物活性多經各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業團隊跟蹤最新的制藥及生命科學研究進展，為您提供*新的活性化合物；
•   與世界各大制藥公司及著名科研機構建立了長期的合作。