Cabozantinib (free base)featured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:200595
CAS#:849217-68-1 (free base)
Description:Cabozantinib, also known as XL-184 or BMS-907351, is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several tyrosine receptor kinases. Specifically, cabozantinib appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression.Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer.
Price and Availability
Cabozantinib (XL184) (free base), purity > 98%, is in stock. The same day shipping out after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 200595Name: Cabozantinib (free base)CAS#: 849217-68-1 (free base)Chemical Formula: C28H24FN3O5Exact Mass: 501.17Molecular Weight: 501.51Elemental Analysis:C, 67.06; H, 4.82; F, 3.79; N, 8.38; O, 15.95
Related CAS #:1140909-48-3 (malate)849217-68-1 (free base)
Synonym:XL-184; XL184; XL 184; BMS 907351; BMS-907351; BMS907351; Cabozantinib, Cabozantinib free base; trade name Cometriq
IUPAC/Chemical Name:N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1- dicarboxamide
InChi Key:ONIQOQHATWINJY-UHFFFAOYSA-N
InChi Code:InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
SMILES Code:O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C=C3
Technical Data
Additional Information
Related CAS#CAS#849217-68-1 (Cabozantinib free base); CAS#1140909-48-3 (Cabozantinib malate salt).
Cabozantinib (Marketed under the tradename Cometriq, formerly known as XL184) is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and has been shown to reduce tumor growth, metastasis, and angiogenesis. It was developed by Exelixis Inc. Cabozantinib was granted orphan-drug status by the U.S. Food and Drug Administration (FDA) in January 2011. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer[2] and it is currently undergoing clinical trials for the treatment of prostate, ovarian, brain, melanoma, breast, non-small cell lung, hepatocellular and kidney cancers. (source: http://en.wikipedia.org/wiki/Cabozantinib).
References
1: Weitzman SP, Cabanillas ME. The treatment landscape in thyroid cancer: a focus on cabozantinib. Cancer Manag Res. 2015 Aug 19;7:265-78. doi: 10.2147/CMAR.S68373. eCollection 2015. Review. PubMed PMID: 26316818; PubMed Central PMCID: PMC4547654.
2: Zhang B, Zhang X, Zhou T, Liu J. Clinical observation of liver cancer patients treated with axitinib and cabozantinib after failed sorafenib treatment: a case report and literature review. Cancer Biol Ther. 2015;16(2):215-8. doi: 10.4161/15384047.2014.962318. Review. PubMed PMID: 25668362; PubMed Central PMCID: PMC4622678.
3: Fay AP, Albiges L, Bellmunt J. Current role of cabozantinib in metastatic castration-resistant prostate cancer. Expert Rev Anticancer Ther. 2015 Feb;15(2):151-6. doi: 10.1586/14737140.2015.1003047. Epub 2015 Jan 14. Review. PubMed PMID: 25586337.
4: Roy S, Narang BK, Rastogi SK, Rawal RK. A novel multiple tyrosine-kinase targeted agent to explore the future perspectives of anti-angiogenic therapy forthe treatment of multiple solid tumors: cabozantinib. Anticancer Agents Med Chem. 2015;15(1):37-47. Review. PubMed PMID: 25181996.
5: Hoy SM. Cabozantinib: a review of its use in patients with medullary thyroid cancer. Drugs. 2014 Aug;74(12):1435-44. doi: 10.1007/s40265-014-0265-x. Review. PubMed PMID: 25056653.
6: Nix NM, Braun K. Cabozantinib for the treatment of metastatic medullary thyroid carcinoma. J Adv Pract Oncol. 2014 Jan;5(1):47-50. Review. PubMed PMID: 25032033; PubMed Central PMCID: PMC4093460.
7: Colombo JR, Wein RO. Cabozantinib for progressive metastatic medullary thyroid cancer: a review. Ther Clin Risk Manag. 2014 May 28;10:395-404. doi: 10.2147/TCRM.S46041. eCollection 2014. Review. PubMed PMID: 24920914; PubMed Central PMCID: PMC4043815.
8: Vaishampayan UN. Development of cabozantinib for the treatment of prostate cancer. Core Evid. 2014 Apr 23;9:61-7. doi: 10.2147/CE.S48498. eCollection 2014.Review. Erratum in: Core Evid. 2014;9:69. PubMed PMID: 24790591; PubMed Central PMCID: PMC4003147.
9: Grüllich C. Cabozantinib: a MET, RET, and VEGFR2 tyrosine kinase inhibitor. Recent Results Cancer Res. 2014;201:207-14. doi: 10.1007/978-3-642-54490-3_12. Review. PubMed PMID: 24756794.
10: Pinto A. Cabozantinib: a novel agent with a dual mechanism of action for castration-resistant prostate carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):219-22. doi: 10.1007/s00280-013-2343-2. Epub 2013 Nov 8. Review. PubMed PMID: 24202668.
11: Karras S, Pontikides N, Krassas GE. Pharmacokinetic evaluation of cabozantinib for the treatment of thyroid cancer. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):507-15. doi: 10.1517/17425255.2013.780028. Review. PubMed PMID: 23488614.
12: Nagilla M, Brown RL, Cohen EE. Cabozantinib for the treatment of advanced medullary thyroid cancer. Adv Ther. 2012 Nov;29(11):925-34. doi: 10.1007/s12325-012-0060-6. Epub 2012 Oct 25. Review. PubMed PMID: 23104465.
13: Bowles DW, Kessler ER, Jimeno A. Multi-targeted tyrosine kinase inhibitors in clinical development: focus on XL-184 (cabozantinib). Drugs Today (Barc). 2011 Nov;47(11):857-68. doi: 10.1358/dot.2011.47.11.1688487. Review. PubMed PMID: 22146228.
14: Durante C, Russo D, Verrienti A, Filetti S. XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413.doi: 10.1517/13543784.2011.559163. Review. PubMed PMID: 21314233.
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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