CAS: 1123837-84-2; N-(3-Fluoro-4-((2-(5-(((2-Methoxyethyl)Amino)Methyl)Pyridin-2-yl)Thieno[3,2-B]Pyridin-7-yl)Oxy)Phenyl)-N-(4-Fluorophenyl)Cyclopropane-1,1-Dicarboxamide
该化合物是一个复杂的有机化合物,具有多功能结构特征.它有一个环丙丙烷二氧基胺核心,其潜在生物活动是显著的.分子中含有氟丙烯原子会加强其脂性,可能会影响其相干特性.该化合物还含有多种芳香和环球性,有助于其与生物目标的潜在相互作用.其含氧乙基乙基乙基和氨基基基组表明有机溶剂中可能溶解性以及氢联结潜力,这可能会影响其再活性和稳定性.该化合物可能对医药化学,特别是药物的研制具有兴趣,并可能影响到其精密性,因为其生物特性可能具有具体的特性.
- 英文名称N-(3-Fluoro-4-((2-(5-(((2-Methoxyethyl)Amino)Methyl)Pyridin-2-yl)Thieno[3,2-B]Pyridin-7-yl)Oxy)Phenyl)-N-(4-Fluorophenyl)Cyclopropane-1,1-Dicarboxamide
- 中文名称司曲替尼
- IUPAC名称N-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
- 其它别名1,1-Cyclopropanedicarboxamide, N-(3-Fluoro-4-((2-(5-(((2-Methoxyethyl)Amino)Methyl)-2-Pyridinyl)Thieno(3,2-B)Pyridin-7-yl)Oxy)Phenyl)-N'-(4-Fluorophenyl)-; Sitravatinib (Usan/inn)
- CAS编号1123837-84-2
- MFCD编号:MFCD28502181
- FDA UNII编号:CWG62Q1VTB
- 分子式:C33H29F2N5O4S分子量:629.69
- 产品CID: 157290
- 同类组份化合物CAS2244864-88-6 (malate)1123837-84-2 (free base)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 沸点833.5±65.0 °C at 760 mmHg
- 闪点457.9±34.3 °C
- 密度1.4±0.1 g/cm3
- pKa:13.17±0.70(预测)
- LogP:6.0
- 折射率1.685
- 蒸汽压0.0±3.1 mmHg at 25°C
- 溶解性Soluble In DMSO (Up To At Least 25 mg/mL), Or In Ethanol (Up To At Least 25 mg/mL)
- 外观形态类白色固体
- 储存条件-20°C
- 产品应用该化合物是一种新型的小分子抑制剂,针对的是S180 SHARCOMA细胞生长(包括C-KIT,PDGFRET,PGFFRAT,C-MET和AXL)的监管中涉及的多受体强力强力抗体性强力性直流体;它明显抑制了驱动力RTK的磷化,从而在体外显出强大的抗扩散效应;在体内,SATRAVATINIB展示了临床前癌症模型中的抗脉搏活动,在目标中隐藏基因变化,如RET,NTRK聚变或CH4Q12放大, 并显示与异基因模型中的IMATINIB和CRIZOTINB相比,肿瘤生长抑制力更大.
上下游产品
Tert-Butyl ((6-(7-(2-Fluoro-4-(1-((4-Fluorophenyl)Carbamoyl)Cyclopropane-1-Carboxamido)Phenoxy)Thieno[3,2-B]Pyridin-2-yl)Pyridin-3-yl)Methyl)(2-Methoxyethyl)Carbamate 1123837-39-74-[[2-[5-[[boc(2-甲氧基乙基)氨基]甲基]-2-吡啶基]-7-噻吩并[3,2-B]吡啶基]氧基]-3-氟苯胺 Tert-Butyl ((6-(7-(4-Amino-2-Fluorophenoxy)Thieno[3,2-B]Pyridin-2-yl)Pyridin-3-yl)Methyl)(2-Methoxyethyl)Carbamate 1123837-34-2
Tert-Butyl ((6-(7-Chlorothieno[3,2-B]Pyridin-2-yl)Pyridin-3-yl)Methyl)(2-Methoxyethyl)Carbamate 1123838-02-7
合成工艺路线路线简述
📜4-氨基-2-氟苯酚盐酸盐置于吡啶,盐酸,氯化亚砜,Potassium Tert-Butylate,Potassium Carbonate,溶剂黄146,三乙胺体系中,用 四氢呋喃,水,二甲基亚砜 用作溶剂,化学反应 12.67H,反应生成司曲替尼
参考文献: Crystalline Form Of A Multi-Tyrosine Kinase Inhibitor,Method Of Preparation,And Use Thereof[fr] Forme Cristalline D'Un Inhibiteur De La Tyrosine Kinase Multiple,Son Procédé De Préparation Et Son Utilisation
标题: Crystalline Form Of A Multi-Tyrosine Kinase Inhibitor,Method Of Preparation,And Use Thereof[fr] Forme Cristalline D'Un Inhibiteur De La Tyrosine Kinase Multiple,Son Procédé De Préparation Et Son Utilisation
摘要:本发明涉及n-(3-氟-4-((2-(5-(((2-甲氧基乙基)氨基甲基)吡啶-2-基)噻吩[3,2-B]吡啶-7-基)氧基)苯基)-N-(4-氟苯基)环丙烷-1,1-二甲酰胺(化合物1)的晶型形式,包括该晶型形式的药物组合物,制备该晶型形式的方法以及使用方法.
海关参考信息
- 2912110000-甲醛
2912120000-乙醛
2922110001-单乙醇胺
2924292000-扑热息痛 - 💡 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
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: Ajadee A, Mahmud S, Hossain MB, Ahmmed R, Ali MA, Reza MS, Sarker SK, Mollah MNH. Screening of differential gene expression patterns through survival analysis for diagnosis, prognosis and therapies of clear cell renal cell carcinoma. PLoS One. 2024 Sep 30;19(9):e0310843. doi: 10.1371/journal.pone.0310843.
2: Li J, Bai Y, Chen Z, Ying J, Guo Y, Fang W, Zhang F, Xiong J, Zhang T, Meng Z, Zhang J, Ren Z, Hao C, Chen Y, Lin X, Pan H, Zhou F, Li X, Yu F, Zhang J, Zhang Z, Qin S. SAFFRON-104: a phase Ib/II study of sitravatinib alone or with tislelizumab in advanced hepatocellular carcinoma and gastric cancer/gastroesophageal junction cancer. Cancer Immunol Immunother. 2024 Sep 5;73(11):219. doi: 10.1007/s00262-024-03806-2.
3: Pant S, Cho BC, Kyriakopoulos CE, Spira A, Tannir N, Werner TL, Yan X, Neuteboom S, Chao R, Goel S. Targeting multiple receptor tyrosine kinases with sitravatinib: A Phase 1b study in advanced renal cell carcinoma and castrate- resistant prostate cancer. Invest New Drugs. 2024 Aug 21. doi: 10.1007/s10637-024-01465-9. Epub ahead of print. 16(12):2253. doi: 10.3390/cancers16122253.
合成参考文献
参考文献:10.1007/13905_2021_14
摘要:Foerster F, Galle PR. Immunotherapy in GI Cancers: Hepatocellular Carcinoma: Perspective. 2022. In: Cancer Immunotherapy.
参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
参考文献:10.1007/16833_2022_15
摘要:Lorenzo Pouso AI, González-Moles MÁ, Ramos-García P, Pérez Sayáns M. The Immunohistochemical Landscape of the Hypoxia-Related Proteins in Oral Squamous Cell Carcinoma. 2022. In: Interdisciplinary Cancer Research.
参考文献:10.1007/13905_2022_32
摘要:Howard FM, Agrawal N, Rosenberg AJ. Clinical Application of Immunotherapy in the Perioperative Management of Head and Neck Cancer. 2022. In: Cancer Immunotherapy.
参考文献:10.1007/978-3-031-40901-1_9
摘要:Brown JT, Jani Y, Master VA, Bilen MA. Neoadjuvant Therapy in Locally Advanced Renal Cell Carcinoma. 2023. In: Integrating Multidisciplinary Treatment for Advanced Renal Cell Carcinoma.
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