CAS: 957054-33-0; Gdc-0941 Dimethanesulfonate
该化合物是一种复杂的有机化合物,其独特的结构特征包括一个含有异氮酸酯混合物的核核心,并代之以一个管状酸和氨基化合物.该化合物通常用于制药研究,特别是由于其生物活性特性而开发潜在的治疗剂.甲烷泡沫盐形式的存在,增强了其溶性和稳定性,使之适合于各种生物实验.其分子结构表明它与生物目标的潜在相互作用,其中可能包括与疾病路径有关的酶或感官.该化合物的合成和特征涉及先进的有机化学技术,而且该化合物在临床前研究中对功效和安全进行严格测试.
- 英文名称Gdc-0941 Dimethanesulfonate
- 中文名称2-(1H-吲唑-4-基)-6-[[4-(甲基磺酰基)-1-哌嗪基]甲基]-4-(4-吗啉基)噻吩并[3,2-d]嘧啶
- IUPAC名称4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine dimethanesulfonate
- 其它别名Pictilisib (Dimethanesulfonate); 2-(1H-Indazol-4-yl)-6-(4-Methanesulfonyl-Piperazin-1-Ylmethyl)-4-Morpholin-4-Yl-Thieno[3,2-D]Pyrimidine Bismesylate; Pictilisib Dimesylate
- CAS编号957054-33-0
- MFCD编号:MFCD12546329
- FDA UNII编号:G3D7HF2GS9
- 分子式:C25H35N7O9S4分子量:705.86
- 产品CID: 2011028
- 同类组份化合物CAS957054-30-7 (free base)957054-33-0 (mesylate)
- 产品分类生物化工 → 抑制剂 → 蛋白酪氨酸激酶
物理性质
MSDS等安全信息
合成工艺路线路线简述
📜4-羟基-2,6-二甲基苯甲腈,甲烷磺酸置于乙醚体系中,用 二氯甲烷,甲醇 作为反应溶剂,化学反应 3.0H,以to Give The Title Compound (2.70G)的收率获得产物2-(1H-吲唑-4-基)-6-[[4-(甲基磺酰基)-1-哌嗪基]甲基]-4-(4-吗啉基)噻吩并[3,2-D]嘧啶
参考文献:Pharmaceutical Compounds
标题:Pharmaceutical Compounds
摘要:本文提供了一种药物组合物,其包括一种药用可接受载体或稀释剂以及作为活性成分的化合物2-(1H-吲唑-4-基)-6-(4-甲磺酰基哌嗪-1-基甲基)-4-吗啉基硫杂[3,2-D]嘧啶双甲磺酸盐.
海关参考信息
- 2902200000-苯
2909110000-乙醚
2921211000-乙二胺
2922110001-单乙醇胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound
专利号:US-2025206735-A1
优先权日:2018-11-16
标题:Synthesis of key intermediate of kras g12c inhibitor compound
专利号:US-12391689-B2
优先权日:2018-11-16
标题 :Synthesis of key intermediate of KRAS G12C inhibitor compound
专利号:EP-3880670-B1
优先权日:2018-11-16
标题 :Improved synthesis of key intermediate of kras g12c inhibitor compound
专利号:EP-4058432-A1
优先权日:2019-11-14
标 题:Improved synthesis of kras g12c inhibitor compound
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: De Wolf E, De Wolf C, Richardson A. ABT-737 and pictilisib synergistically enhance pitavastatin-induced apoptosis in ovarian cancer cells. Oncol Lett. 2018 Feb;15(2):1979-1984. doi: 10.3892/ol.2017.7516. Epub 2017 Dec 5.
2: Keegan NM, Gleeson JP, Hennessy BT, Morris PG. PI3K inhibition to overcome endocrine resistance in breast cancer. Expert Opin Investig Drugs. 2018 Jan;27(1):1-15. doi: 10.1080/13543784.2018.1417384. Epub 2018 Jan 6. Review. doi: 10.1038/s41389-017-0004-8. doi: 10.1016/j.ejca.2017.08.027. Epub 2017 Oct 6. doi: 10.18632/oncotarget.19194. eCollection 2017 Sep 8.
7: Chen J, Guo J, Cui X, Dai Y, Tang Z, Qu J, Raj JU, Hu Q, Gou D. The Long Noncoding RNA LnRPT Is Regulated by PDGF-BB and Modulates the Proliferation of Pulmonary Artery Smooth Muscle Cells. Am J Respir Cell Mol Biol. 2018 Feb;58(2):181-193. doi: 10.1165/rcmb.2017-0111OC. doi: 10.1158/1078-0432.CCR-17-0033. Epub 2017 Aug 14.
合成参考文献
参考文献:10.1021/jm2009327
摘要:Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, Nonomiya J, Pang J, Pegg N, Prior WW, Rouge L, Salphati L, Sampath D, Tian Q, Tsui V, Wan NC, Wang S, Wei B, Wiesmann C, Wu P, Zhu BY, Olivero A. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem. 2011 Nov 10;54(21):7579–87. doi: 10.1021/jm2009327.
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