Navitoclaxfeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:201970
CAS#:923564-51-6
Description:Navitoclax, also known as ABT-263, is an orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w.
Price and Availability
Navitoclax, purity > 98%, is in stock. The same day shipping after order is received.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 201970Name: NavitoclaxCAS#: 923564-51-6Chemical Formula: C47H55ClF3N5O6S3Exact Mass: 973.29551Molecular Weight: 974.61Elemental Analysis:C, 57.92; H, 5.69; Cl, 3.64; F, 5.85; N, 7.19; O, 9.85; S, 9.87
Synonym:ABT 263; ABT-263; ABT263; Navitoclax
IUPAC/Chemical Name:(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
InChi Key:JLYAXFNOILIKPP-KXQOOQHDSA-N
InChi Code:InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1
SMILES Code:O=C(NS(=O)(C1=CC=C(N[C@H](CCN2CCOCC2)CSC3=CC=CC=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C4=CC=C(N5CCN(CC6=C(C7=CC=C(Cl)C=C7)CCC(C)(C)C6)CC5)C=C4
Technical Data
Additional Information
Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance.
References
1: Kaefer A, Yang J, Noertersheuser P, Mensing S,Humerickhouse R, Awni W, Xiong H. Mechanism-based pharmacokinetic/pharmacodynamicmeta-analysis of navitoclax (ABT-263) induced thrombocytopenia. CancerChemother Pharmacol. 2014 Sep;74(3):593-602. doi:10.1007/s00280-014-2530-9. Epub 2014 Jul 23. PubMed PMID: 25053389.
2: Yang J, Pradhan RS, Rosen LS, Graham AM, Holen KD, Xiong H. Effect ofrifampin on the pharmacokinetics, safety and tolerability of navitoclax(ABT-263), a dual inhibitor of Bcl-2 and Bcl-X(L) , in patients withcancer. J Clin Pharm Ther. 2014 Jul 22. doi: 10.1111/jcpt.12193. [Epubahead of print] PubMed PMID: 25047139.
3: Wei X, Zhou P, Lin X, Lin Y, Wu S, Diao P, Xie H, Xie K, Tang P.MLN2238 synergizes BH3 mimetic ABT-263 in castration-resistant prostatecancer cells by induction of NOXA. Tumour Biol. 2014 Jul 17. [Epub aheadof print] PubMed PMID: 25027405.
4: Suryani S, Carol H, Chonghaile TN, Frismantas V, Sarmah C, High L,Bornhauser B, Cowley MJ, Szymanska B, Evans K, Boehm I, Tonna E, JonesL, Manesh DM, Kurmasheva RT, Billups C, Kaplan W, Letai A, Bourquin JP,Houghton PJ, Smith MA, Lock RB. Cell and Molecular Determinants of InVivo Efficacy of the BH3 Mimetic ABT-263 against Pediatric AcuteLymphoblastic Leukemia Xenografts. Clin Cancer Res. 2014 Sep1;20(17):4520-31. doi: 10.1158/1078-0432.CCR-14-0259. Epub 2014 Jul 10.PubMed PMID: 25013123; PubMed Central PMCID: PMC4154988.
5: Polier G, Giaisi M, Köhler R, Müller WW, Lutz C, Buss EC, Krammer PH,Li-Weber M. Targeting CDK9 by wogonin and related natural flavonespotentiates the anti-cancer efficacy of the Bcl-2 family inhibitorABT-263. Int J Cancer. 2014 Jun 4. doi: 10.1002/ijc.29009. [Epub aheadof print] PubMed PMID: 24895203.
6: Vlahovic G, Karantza V, Wang D, Cosgrove D, Rudersdorf N, Yang J,Xiong H, Busman T, Mabry M. A phase I safety and pharmacokinetic studyof ABT-263 in combination with carboplatin/paclitaxel in the treatmentof patients with solid tumors. Invest New Drugs. 2014 Oct;32(5):976-84.doi: 10.1007/s10637-014-0116-3. Epub 2014 Jun 5. PubMed PMID: 24894650.
7: Wang X, Gu Z, Li G, Zhang S, Cao Z, Yang Z, Liu G. Norcantharidinenhances ABT-263-mediated anticancer activity in neuroblastoma cells byupregulation of Noxa. Oncol Rep. 2014 Aug;32(2):716-22. doi:10.3892/or.2014.3228. Epub 2014 May 30. PubMed PMID: 24891300.
8: Wang B, Ni Z, Dai X, Qin L, Li X, Xu L, Lian J, He F. The Bcl-2/xLinhibitor ABT-263 increases the stability of Mcl-1 mRNA and protein inhepatocellular carcinoma cells. Mol Cancer. 2014 Apr 30;13:98. doi:10.1186/1476-4598-13-98. PubMed PMID: 24779770; PubMed Central PMCID:PMC4021276.
9: Li J, Chen Y, Wan J, Liu X, Yu C, Li W. ABT-263 enhances sorafenib-inducedapoptosis associated with Akt activity and the expression of Bax andp21((CIP1/WAF1)) in human cancer cells. Br J Pharmacol. 2014Jul;171(13):3182-95. doi: 10.1111/bph.12659. PubMed PMID: 24571452;PubMed Central PMCID: PMC4080973.
10: Choo EF, Boggs J, Zhu C, Lubach JW, Catron ND, Jenkins G, Souers AJ,Voorman R. The role of lymphatic transport on the systemicbioavailability of the Bcl-2 protein family inhibitors navitoclax(ABT-263) and ABT-199. Drug Metab Dispos. 2014 Feb;42(2):207-12. doi:10.1124/dmd.113.055053. Epub 2013 Nov 8. PubMed PMID: 24212376.
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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