Obatoclax mesylatefeatured
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:202050
CAS#:803712-79-0 (mesylate)
Description:Obatoclax, also known as GX 015-070, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon.
Price and Availability
Obatoclax mesylate, 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#: 202050Name: Obatoclax mesylateCAS#: 803712-79-0 (mesylate)Chemical Formula: C21H23N3O4SExact Mass: 317.15281Molecular Weight: 413.49002Elemental Analysis: C, 61.00; H, 5.61; N, 10.16; O, 15.48; S, 7.75
Related CAS #:803712-67-6 (free base)803712-79-0 (mesylate)
Synonym:Obatoclax; Obatoclax mesylate; GX 015-070; GX015-070; GX-015-070; GX 015070; GX015070; GX-015070; GX 05-070; GX15070MS.
IUPAC/Chemical Name:(Z)-2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-1H-indole methanesulfonate
InChi Key:ZFKXDVMHNXPEIY-PEZBNFGJSA-N
InChi Code:InChI=1S/C20H19N3O.CH4O3S/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17;1-5(2,3)4/h4-11,21-22H,1-3H3;1H3,(H,2,3,4)/b19-10-;
SMILES Code:COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=CC4=C(C)C=C(C)N4.CS(=O)(O)=O
Technical Data
Additional Information
Related CAS#803712-67-6 (Obatoclax free base)803712-79-0(Obatoclax mesylate)
References
1: DÃaz de Greñu B, Hernández PI, Espona M, QuiñoneroD, Light ME, Torroba T, Pérez-Tomás R, Quesada R. Synthetic ProdiginineObatoclax (GX15-070) and Related Analogues: Anion Binding, TransmembraneTransport, and Cytotoxicity Properties. Chemistry. 2011 Nov 9. doi:10.1002/chem.201101547. [Epub ahead of print] PubMed PMID: 22069220.
2: Lieber J, Ellerkamp V, Wenz J, Kirchner B, Warmann SW, Fuchs J,Armeanu-Ebinger S. Apoptosis sensitizers enhance cytotoxicity inhepatoblastoma cells. Pediatr Surg Int. 2011 Oct 5. [Epub ahead ofprint] PubMed PMID: 21971946.
3: MartÃnez-Paniagua MA, Baritaki S, Huerta-Yepez S, Ortiz-Navarrete VF,González-Bonilla C, Bonavida B, Vega MI. Mcl-1 and YY1 inhibition andinduction of DR5 by the BH3-mimetic Obatoclax (GX15-070) contribute inthe sensitization of B-NHL cells to TRAIL apoptosis. Cell Cycle. 2011Aug 15;10(16):2792-805. Epub 2011 Aug 15. PubMed PMID: 21822052.
4: Jóna A, Khaskhely N, Buglio D, Shafer JA, Derenzini E, Bollard CM,Medeiros LJ, Illés A, Ji Y, Younes A. The histone deacetylase inhibitorentinostat (SNDX-275) induces apoptosis in Hodgkin lymphoma cells andsynergizes with Bcl-2 family inhibitors. Exp Hematol. 2011Oct;39(10):1007-1017.e1. doi: 10.1016/j.exphem.2011.07.002. Epub 2011Jul 20. PubMed PMID: 21767511; PubMed Central PMCID: PMC3177003.
5: Acoca S, Cui Q, Shore GC, Purisima EO. Molecular dynamics study ofsmall molecule inhibitors of the Bcl-2 family. Proteins. 2011Sep;79(9):2624-36. doi: 10.1002/prot.23083. Epub 2011 Jun 30. PubMedPMID: 21721047.
6: Herishanu Y, Gibellini F, Njuguna N, Hazan-Halevy I, Farooqui M, BernS, Keyvanfar K, Lee E, Wilson W, Wiestner A. Activation of CD44, areceptor for extracellular matrix components, protects chroniclymphocytic leukemia cells from spontaneous and drug induced apoptosisthrough MCL-1. Leuk Lymphoma. 2011 Sep;52(9):1758-69. Epub 2011 Jun 8.PubMed PMID: 21649540.
7: Paik PK, Rudin CM, Pietanza MC, Brown A, Rizvi NA, Takebe N, TravisW, James L, Ginsberg MS, Juergens R, Markus S, Tyson L, Subzwari S, KrisMG, Krug LM. A phase II study of obatoclax mesylate, a Bcl-2 antagonist,plus topotecan in relapsed small cell lung cancer. Lung Cancer. 2011Dec;74(3):481-5. Epub 2011 May 26. PubMed PMID: 21620511.
8: Brem EA, Thudium K, Khubchandani S, Tsai PC, Olejniczak SH, Bhat S,Riaz W, Gu J, Iqbal A, Campagna R, Knight J, Mavis C, Hoskin P, Deeb G,Gibbs JF, Fetterly G, Czuczman MS, Hernandez-Ilizaliturri FJ. Distinctcellular and therapeutic effects of obatoclax in rituximab-sensitive and-resistant lymphomas. Br J Haematol. 2011 Jun;153(5):599-611. doi:10.1111/j.1365-2141.2011.08669.x. Epub 2011 Apr 15. PubMed PMID:21492126; PubMed Central PMCID: PMC3092002.
9: Dean EJ, Cummings J, Roulston A, Berger M, Ranson M, Blackhall F,Dive C. Optimization of circulating biomarkers of obatoclax-induced celldeath in patients with small cell lung cancer. Neoplasia. 2011Apr;13(4):339-47. PubMed PMID: 21472138; PubMed Central PMCID:PMC3071082.
10: Heidari N, Hicks MA, Harada H. GX15-070 (obatoclax) overcomesglucocorticoid resistance in acute lymphoblastic leukemia throughinduction of apoptosis and autophagy. Cell Death Dis. 2010 Sep 16;1:e76.PubMed PMID: 21364679; PubMed Central PMCID: PMC3032343.
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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