Axitinibfeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:200400
CAS#:319460-85-0
Description:Axitinib, also known as AG013736, is an orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived growth factor receptor (PDGF), thereby exerting an anti-angiogenic effect. A xitinib has received FDA (27 January 2012), EMA (13 September 2012), MHRA (3 September 2012) and TGA (26 July 2012) approval for use as a treatment for renal cell carcinoma.
Price and Availability
Axitinib, purity > 98%, is in stock. The same day shipping out after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 200400Name: AxitinibCAS#: 319460-85-0Chemical Formula: C22H18N4OSExact Mass: 386.12013Molecular Weight: 386.47Elemental Analysis:C, 68.37; H, 4.69; N, 14.50; O, 4.14; S, 8.30
Synonym:AG013736; AG 013736; AG-013736; Axitinib; Brand name: Inlyta.
IUPAC/Chemical Name:(E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide
InChi Key:RITAVMQDGBJQJZ-FMIVXFBMSA-N
InChi Code:InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
SMILES Code:O=C(NC)C1=CC=CC=C1SC2=CC3=C(C=C2)C(/C=C/C4=NC=CC=C4)=NN3
Technical Data
Additional Information
Axitinib (also known as AG013736) is a small molecule tyrosine kinase inhibitor under development by Pfizer. It inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117). It has been shown to significantly inhibit growth of breast cancer in xenograft models and has been successful in trials with renal cell carcinoma (RCC) and several other tumor types.Axitinib is a white to light-yellow powder with a pKa of 4.8. The solubility of axitinib in aqueous media over the range pH 1.1 to pH 7.8 is in excess of 0.2 μg/mL. The partition coefficient (n-octanol/water) is 3.5. A Phase II clinical trial showed good response in combination chemotherapy with Gemcitabine for advanced pancreatic cancer. However, Pfizer reported on January 30, 2009 that Phase III clinical trials of the drug when used in combination with Gemcitabine showed no evidence of improved survival rates over treatments using Gemcitabine alone for advanced pancreatic cancer and halted the trial. see http://en.wikipedia.org/wiki/Axitinib.
References
1: Gunnarsson O, Pfanzelter NR, Cohen RB, Keefe SM.Evaluating the safety and efficacy of axitinib in the treatment ofadvanced renal cell carcinoma. Cancer Manag Res. 2015 Feb 11;7:65-73.doi: 10.2147/CMAR.S74202. eCollection 2015. Review. PubMed PMID:25709499; PubMed Central PMCID: PMC4334173.
2: Tzogani K, Skibeli V, Westgaard I, Dalhus M, Thoresen H, Slot KB,Damkier P, Hofland K, Borregaard J, Ersbøll J, Salmonson T, Pieters R,Sylvester R, Mickisch G, Bergh J, Pignatti F. The European MedicinesAgency Approval of Axitinib (Inlyta) for the Treatment of Advanced RenalCell Carcinoma After Failure of Prior Treatment With Sunitinib or aCytokine: Summary of the Scientific Assessment of the Committee forMedicinal Products for Human Use. Oncologist. 2015 Feb;20(2):196-201.Epub 2015 Jan 23. Review. PubMed PMID: 25616431; PubMed Central PMCID:PMC4319625.
3: Borst DL, Arruda LS, MacLean E, Pithavala YK, Morgado JE. Commonquestions regarding clinical use of axitinib in advanced renal cellcarcinoma. Am J Health Syst Pharm. 2014 Jul 1;71(13):1092-6. doi:10.2146/ajhp130581. Review. PubMed PMID: 24939498.
4: Verzoni E, Grassi P, Testa I, Iacovelli R, Biondani P, Garanzini E,De Braud F, Procopio G. Targeted treatments in advanced renal cellcarcinoma: focus on axitinib. Pharmgenomics Pers Med. 2014 Mar27;7:107-16. doi: 10.2147/PGPM.S37098. eCollection 2014. Review. PubMedPMID: 24715765; PubMed Central PMCID: PMC3977458.
5: Bracarda S, Castellano D, Procopio G, Sepúlveda JM, Sisani M, VerzoniE, Schmidinger M. Axitinib safety in metastatic renal cell carcinoma:suggestions for daily clinical practice based on case studies. ExpertOpin Drug Saf. 2014 Apr;13(4):497-510. doi:10.1517/14740338.2014.888413. Review. PubMed PMID: 24641566.
6: Akaza H, Fukuyama T. Axitinib for the treatment of advanced renalcell carcinoma. Expert Opin Pharmacother. 2014 Feb;15(2):283-97. doi:10.1517/14656566.2014.868436. Epub 2013 Dec 13. Review. PubMed PMID:24328549.
7: Gross-Goupil M, François L, Quivy A, Ravaud A. Axitinib: a review ofits safety and efficacy in the treatment of adults with advanced renalcell carcinoma. Clin Med Insights Oncol. 2013 Oct 29;7:269-77. doi:10.4137/CMO.S10594. Review. PubMed PMID: 24250243; PubMed Central PMCID:PMC3825605.
8: Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK.Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. Review. PubMed PMID:23677771.
9: Qi WX, He AN, Shen Z, Yao Y. Incidence and risk of hypertension witha novel multi-targeted kinase inhibitor axitinib in cancer patients: asystematic review and meta-analysis. Br J Clin Pharmacol. 2013Sep;76(3):348-57. doi: 10.1111/bcp.12149. Review. PubMed PMID: 23617405;PubMed Central PMCID: PMC3769663.
10: King JW, Lee SM. Axitinib for the treatment of advancednon-small-cell lung cancer. Expert Opin Investig Drugs. 2013Jun;22(6):765-73. doi: 10.1517/13543784.2013.775243. Epub 2013 Mar 1.Review. PubMed PMID: 23452008.
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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