CAS: 649735-46-6; (R)-1-((4-((4-Fluoro-2-Methyl-1H-Indol-5-yl)Oxy)-5-Methylpyrrolo[2,1-F][1,2,4]Triazin-6-yl)Oxy)Propan-2-Ol
该化合物是一个小分子,主要作为血管内皮生长因子(VEGF)和纤维生长因子(FGF)的双重抑制剂,主要针对各种固态肿瘤,被归类为抗癌剂,具体针对各种固态肿瘤;该化合物展示了一个复杂的化学结构,通过抑制与这些途径相关的受体性强血清血清素激素细胞酶,干扰肿瘤的产生和生长;Brivanib在临床试验中接受了调查,以了解其在治疗肝细胞癌和其他恶性肿瘤等疾病方面的功效;其药用植物基因特性包括口服生物利用率,主要在肝脏中进行代谢;该物质显示出一系列生物活动,包括对癌症细胞的抗生素效应;但是,与许多有针对性的疗法一样,它也可能产生副作用,需要在治疗期间进行仔细监测.总的来说,Brivanib是定向癌症疗法发展的重大进展.
- 英文名称(R)-1-((4-((4-Fluoro-2-Methyl-1H-Indol-5-yl)Oxy)-5-Methylpyrrolo[2,1-F][1,2,4]Triazin-6-yl)Oxy)Propan-2-Ol
- 中文名称1-[[4-[(4-氟-2-甲基-1H-吲哚-5-基)氧基]-5-甲基吡咯并[2,1-f][1,2,4]三嗪-6-基]氧基]-2-丙醇
- IUPAC名称(R)-1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-ol
- 其它别名1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol; Brivanib; Tyrosine Kinase Inhibitor; (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yloxy)propan-2-ol; 2-Propanol, 1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yl)oxy)-, (2R)-
- CAS编号649735-46-6
- MFCD编号:MFCD13194684
- EINECS号:639-685-1
- FDA UNII编号:DDU33B674I
- 分子式:C19H19FN4O3分子量:370.38
- 产品CID: 2512088
- 同类组份化合物CAS649735-46-6649735-63-7 (alaninate)
- 产品分类生物化工 → 氨基酸及其衍生物 → 酪氨酸类衍生物
物理性质
- 密度1.42
- pKa:14.18±0.20(预测)
- PSA:84.67
- LogP:3.5184
- 折射率1.66
- 溶解性Insoluble In H2O; ≥18.5 mg/mL In DMSO; ≥3.39 mg/mL In Etoh With Ultrasonic
- 外观形态白色至浅棕色黄色粉末
- 储存条件储存在 -20°C
- 产品应用该化合物是VEGFR2 (IC50=25 NM)的ATP竞争抑制剂,对VEGBFR-1和FGFFR1有中度抑制性活动,对PDGF FR-Β有超过240倍的选择性.它表明对VGF刺激的HUVEC(IC50 =40 NM)和FFG刺激型HVEVEC (IC 50= = 276 NM),对肿瘤细胞线的细胞毒性较低,具有强大的抗细胞毒性.在VEGFRFR2(IC50)和 FGFM)模型中,BRIVANIB显示出重要的抗细胞瘤活动,包括H3396和肝细胞癌(HC)模型,在口服剂量为60和90 毫克/千克时分别达到85%和97%的肿瘤生长抑制作用.它抑制了肿瘤生长,抑制VEEG FFR-2的磷酸,并表明治疗肝细胞肿瘤的功效.BRIWANNIBANNIB已进入第3阶段临床试验阶段.
MSDS等安全信息
欧盟法规
C&L通报上下游产品
4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-ol (R)-propylene oxide 4-fluoro-2-methyl-1H-indol-5-ol 4-Phenoxy-5-methyl-6-hydroxypyrrolo[2,1-f][1,2,4]triazine (S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-(benzyloxycarbonylamino)propanoate合成工艺路线路线简述
📜6-(Benzyloxy)-5-Methylpyrrolo[2,1-F][1,2,4]Triazin-4-Ol置于palladium On Activated Charcoal 甲酸铵,Sodium Hydride,三乙胺,N,N-二异丙基乙胺,三氯氧磷体系中,用 乙醇,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 8.5H,反应生成 布立尼布
参考文献:Discovery And Preclinical Studies Of (R)-1-(4-(4-Fluoro-2-Methyl-1H-Indol-5-Yloxy)-5-Methylpyrrolo[2,1-F][1,2,4]Triazin-6-Yloxy)Propan-2-Ol (Bms-540215),An In Vivo Active Potent Vegfr-2 Inhibitor
标题:Discovery And Preclinical Studies Of (R)-1-(4-(4-Fluoro-2-Methyl-1H-Indol-5-Yloxy)-5-Methylpyrrolo[2,1-F][1,2,4]Triazin-6-Yloxy)Propan-2-Ol (Bms-540215),An In Vivo Active Potent Vegfr-2 Inhibitor
摘要:A Series Of Substituted 4-(4-Fluoro-1H-Indol-5-Yloxy)Pyrrolo-[2,1-F][1,2,4]Triazine-Based Inhibitors Of Vascular Endothelial Growth Factor Receptor-2 Kinase Is Reported. Structure-Activity Relationship Studies Revealed That A Methyl Group At The 5-Position And A Substituted Alkoxy Group At The 6-Position Of The Pyrrolo[2,1-F][1,2,4]Triazine Core Gave Potent Compounds. Biochemical Potency,Kinase Selectivity,And Pharmacokinetics Of The Series Were Optimized And In Vitro Safety Liabilities Were Minimized To Afford Bms-540215 (12). Which Demonstrated Robust Preclinical In Vivo Activity In Human Tumor Xenograft Models. The L-Alanine Prodrug Of 12,Bms-582664 (21),Is Currently Under Evaluation In Clinical Trials For The Treatment Of Solid Tumors.
DOI:10.1021/jm051106D
海关参考信息
- 2905122000-异丙醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇
2908199090-其他酚的卤化衍生物 - 💡 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: Diaz-Padilla I, Siu LL. Brivanib alaninate for cancer. Expert Opin Investig Drugs. 2011 Apr;20(4):577-86. doi: 10.1517/13543784.2011.565329. Epub 2011 Mar 11. 8(9):1083-90. doi: 10.2217/fon.12.104.
170:105721. doi: 10.1016/j.phrs.2021.105721. Epub 2021 Jun 8. 30(11):4477-83. 235(2):1259-1273. doi: 10.1002/jcp.29041. Epub 2019 Jul 4. 31(28):3483-6. doi: 10.1200/JCO.2013.49.7941. Epub 2013 Aug 26. 120(6):601-611. doi: 10.1038/s41416-018-0375-4. Epub 2019 Feb 15.
8: Hofman J, Sorf A, Vagiannis D, Sucha S, Kammerer S, Küpper JH, Chen S, Guo L, Ceckova M, Staud F. Brivanib Exhibits Potential for Pharmacokinetic Drug-Drug Interactions and the Modulation of Multidrug Resistance through the Inhibition of Human ABCG2 Drug Efflux Transporter and CYP450 Biotransformation Enzymes. Mol Pharm. 2019 Nov 4;16(11):4436-4450. doi: 10.1021/acs.molpharmaceut.9b00361. Epub 2019 Oct 21. 31(28):3509-16. doi: 10.1200/JCO.2012.47.3009. Epub 2013 Aug 26. 9(4):e92273. doi: 10.1371/journal.pone.0092273. Erratum in: PLoS One. 2015;10(11):e0142355.
合成参考文献
摘要:Zhang, F.-G.; Ma, J.-A., Science of Synthesis: Knowledge Updates, (2025) 2.
参考文献:10.1186/1756-9966-31-103
摘要:Brunello E, Brunelli M, Bogina G, Caliò A, Manfrin E, Nottegar A, Vergine M, Molino A, Bria E, Massari F, Tortora G, Cingarlini S, Pedron S, Chilosi M, Zamboni G, Miller K, Martignoni G, Bonetti F. FGFR-1 amplification in metastatic lymph-nodal and haematogenous lobular breast carcinoma. Journal of Experimental & Clinical Cancer Research. 2012 Dec 27;31(1):103. doi: 10.1186/1756-9966-31-103.
参考文献:10.1158/1535-7163.mct-12-0275-t
摘要:Bello E, Taraboletti G, Colella G, Zucchetti M, Forestieri D, Licandro SA, Berndt A, Richter P, D'Incalci M, Cavalletti E, Giavazzi R, Camboni G, Damia G. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131–40. doi: 10.1158/1535-7163.mct-12-0275-t.
参考文献:10.1007/s10637-014-0113-6
摘要:Kim CA, Price-Hiller J, Chu QS, Tankel K, Hennig R, Sawyer MB, Spratlin JL. Atypical reversible posterior leukoencephalopathy syndrome (RPLS) induced by cediranib in a patient with metastatic rectal cancer. Invest New Drugs. 2014 Oct;32(5):1036–45. doi: 10.1007/s10637-014-0113-6.
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