Foretinibfeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:201372
CAS#:849217-64-7
Description:Foretinib, also known as XL880 and GSK1363089, is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers.
Price and Availability
Foretinib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 201372Name: ForetinibCAS#: 849217-64-7Chemical Formula: C34H34F2N4O6Exact Mass: 632.24464Molecular Weight: 632.65377Elemental Analysis: C, 64.55; H, 5.42; F, 6.01; N, 8.86; O, 15.17
Synonym:XL880; XL 880; XL-880; GSK1363089; GSK 1363089; GSK-1363089; GSK089; EXEL2880; Foretinib.
IUPAC/Chemical Name:N-[3-fluoro-4-({6-methoxy-7-[3-(morpholin-4-yl)propoxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
InChi Key:CXQHYVUVSFXTMY-UHFFFAOYSA-N
InChi Code:InChI=1S/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42)
SMILES Code:O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OCCCN6CCOCC6)=C(OC)C=C45)C(F)=C3
Technical Data
Additional Information
References
1: Bénard J. [ROS1 fusion proteins, targets offoretinib]. Bull Cancer. 2014 Jan 1;101(1):4. French. PubMed PMID:24649496.
2: Davare MA, Saborowski A, Eide CA, Tognon C, Smith RL, Elferich J,Agarwal A, Tyner JW, Shinde UP, Lowe SW, Druker BJ. Foretinib is apotent inhibitor of oncogenic ROS1 fusion proteins. Proc Natl Acad Sci US A. 2013 Nov 26;110(48):19519-24. doi: 10.1073/pnas.1319583110. Epub2013 Nov 11. PubMed PMID: 24218589; PubMed Central PMCID: PMC3845150.
3: Shah MA, Wainberg ZA, Catenacci DV, Hochster HS, Ford J, Kunz P, LeeFC, Kallender H, Cecchi F, Rabe DC, Keer H, Martin AM, Liu Y, Gagnon R,Bonate P, Liu L, Gilmer T, Bottaro DP. Phase II study evaluating 2dosing schedules of oral foretinib (GSK1363089), cMET/VEGFR2 inhibitor,in patients with metastatic gastric cancer. PLoS One. 2013;8(3):e54014.doi: 10.1371/journal.pone.0054014. Epub 2013 Mar 14. PubMed PMID:23516391; PubMed Central PMCID: PMC3597709.
4: Logan TF. Foretinib (XL880): c-MET inhibitor with activity inpapillary renal cell cancer. Curr Oncol Rep. 2013 Apr;15(2):83-90. doi:10.1007/s11912-013-0299-3. Review. PubMed PMID: 23408121.
5: Choueiri TK, Vaishampayan U, Rosenberg JE, Logan TF, Harzstark AL,Bukowski RM, Rini BI, Srinivas S, Stein MN, Adams LM, Ottesen LH,Laubscher KH, Sherman L, McDermott DF, Haas NB, Flaherty KT, Ross R,Eisenberg P, Meltzer PS, Merino MJ, Bottaro DP, Linehan WM, SrinivasanR. Phase II and biomarker study of the dual MET/VEGFR2 inhibitorforetinib in patients with papillary renal cell carcinoma. J Clin Oncol.2013 Jan 10;31(2):181-6. doi: 10.1200/JCO.2012.43.3383. Epub 2012 Dec 3.PubMed PMID: 23213094; PubMed Central PMCID: PMC3532390.
6: Shapiro GI, McCallum S, Adams LM, Sherman L, Weller S, Swann S, KeerH, Miles D, Müller T, Lorusso P. A Phase 1 dose-escalation study of thesafety and pharmacokinetics of once-daily oral foretinib, a multi-kinaseinhibitor, in patients with solid tumors. Invest New Drugs. 2013Jun;31(3):742-50. doi: 10.1007/s10637-012-9881-z. Epub 2012 Oct 6.PubMed PMID: 23054208.
7: Seiwert T, Sarantopoulos J, Kallender H, McCallum S, Keer HN,Blumenschein G Jr. Phase II trial of single-agent foretinib (GSK1363089)in patients with recurrent or metastatic squamous cell carcinoma of thehead and neck. Invest New Drugs. 2013 Apr;31(2):417-24. doi:10.1007/s10637-012-9861-3. Epub 2012 Aug 24. PubMed PMID: 22918720;PubMed Central PMCID: PMC3589657.
8: Huynh H, Ong R, Soo KC. Foretinib demonstrates anti-tumor activityand improves overall survival in preclinical models of hepatocellularcarcinoma. Angiogenesis. 2012 Mar;15(1):59-70. doi:10.1007/s10456-011-9243-z. Epub 2011 Dec 21. PubMed PMID: 22187171.
9: Dufies M, Jacquel A, Robert G, Cluzeau T, Puissant A, Fenouille N,Legros L, Raynaud S, Cassuto JP, Luciano F, Auberger P. Mechanism ofaction of the multikinase inhibitor Foretinib. Cell Cycle. 2011 Dec1;10(23):4138-48. doi: 10.4161/cc.10.23.18323. Epub 2011 Dec 1. PubMedPMID: 22101270.
10: Kataoka Y, Mukohara T, Tomioka H, Funakoshi Y, Kiyota N, Fujiwara Y,Yashiro M, Hirakawa K, Hirai M, Minami H. Foretinib (GSK1363089), amulti-kinase inhibitor of MET and VEGFRs, inhibits growth of gastriccancer cell lines by blocking inter-receptor tyrosine kinase networks.Invest New Drugs. 2012 Aug;30(4):1352-60. doi:10.1007/s10637-011-9699-0. Epub 2011 Jun 8. PubMed PMID: 21655918.
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(ResearchTrianglePark,简称RTP),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中 文美帝药库医药科技公司创立于2008年总部位于美国东海岸
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造,销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业,医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derivedRNA)与tracrRNA(trans-activatingRNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
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