CAS: 1457983-28-6; 8-Bromo-2-((1-Methylpiperidin-4-yl)Amino)-4-((4-Phenoxyphenyl)Amino)Pyrido[4,3-D]Pyrimidin-5(6H)-One
- 英文名称8-Bromo-2-((1-Methylpiperidin-4-yl)Amino)-4-((4-Phenoxyphenyl)Amino)Pyrido[4,3-D]Pyrimidin-5(6H)-One
- 中文名称8-溴-2-[(1-甲基-4-哌啶基)氨基]-4-[(4-苯氧基苯基)氨基]吡啶并[4,3-d]嘧啶-5(6H)-酮
- IUPAC名称8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one
- 其它别名38-Bromo-11-Methyl-6-Oxa-2,4-Diaza-3(2,4)-Pyrido[4,3-D]Pyrimidina-1(4)-Piperidina-5(1,4),7(1)-Dibenzenaheptaphan-35(36H)-One; 8-Bromo-2-[(1-Methyl-4-Piperidinyl)Amin
- CAS编号1457983-28-6
- MFCD编号:MFCD28167815
- FDA UNII编号:B06W426B66
- 分子式:C25H25BrN6O2分子量:521.42
- 产品CID: 692206
- 同类组份化合物CAS1457983-28-6 (free base)1457983-33-3 (HCl)
- 产品分类生物化工 → 抑制剂 → 血管生成(Angiogenesis)
物理性质
- 密度1.487±0.06 g/cm3
- pKa:8.32±0.40(预测)
- PSA:95.17
- LogP:2.86
- 折射率1.701
- 溶解性≥26.05 mg/mL In DMSO; Insoluble In Etoh; Insoluble In H2O
- 外观形态白色至类白色固体
- 储存条件储存在 -20°C
- 产品应用该化合物是一种新型和强效FLT3抑制剂,其IC50值分别为0.4纳米,0.6纳米M和1纳米M,分别针对FLTD3(WT),FL3(D835Y)和MER,其抗抗其他强暴性顺流体的活性较低,它有效抑制了在RS4-11细胞中显示FLT3-WT和MV4-4-11和MMLM-14内存放FLD3-ITD的M4-LTT3-11 和MOLM-14细胞体中显示的FLTI3自动光谱片3-IDT/N676D,ILT-3-D8335Y/N676D等抗药性细胞中的FLFT3-D3抗药性的强力(IC50 < 10纳米M),在BAFF3细胞中也显示出抗力抗力的抗力.
合成工艺路线路线简述
海关参考信息
- 2933310010-吡啶
2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物
2918290000-其他含酚基羧酸 - 💡 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-11384076-B2
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors
发明人：MAHBOOBI SIAVOSH; SELLMER ANDREAS; PONGRATZ HERWIG; PILSL BERNARDETTE; KRÄMER OLIVER; KINDLER THOMAS; BEYER MANDY
权利人:UNIV REGENSBURG; UNIV DER JOHANNES GUTENBERG UNIV MAINZ
摘要:The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.
专利号:US-2020190075-A1
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors
专利号:EP-3668867-B1
优先权日:2017-08-18
标 题 :Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors
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: Lee HK, Kim HW, Lee IY, Lee J, Lee J, Jung DS, Lee SY, Park SH, Hwang H, Choi JS, Kim JH, Kim SW, Kim JK, Cools J, Koh JS, Song HJ. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19. doi: 10.1182/blood-2013-04-493916. Epub 2014 Feb 14.
合成参考文献
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.
📝 需求与反馈
尽可能描述清楚需求与问题信息
