CAS: 1421783-64-3; 3-((1H-Pyrazolo[3,4-B]Pyridin-5-yl)Ethynyl)-4-Methyl-N-(4-((4-Methylpiperazin-1-yl)Methyl)-3-(Trifluoromethyl)Phenyl)Benzamide Dimethanesulfonate
该化合物是一种针对BCR-ABL1的小型分子性激素性抑制剂,包括T315I突变,它对第一和第二代抑制剂具有抗药性,主要为治疗慢性类流体白血病(CML)和费城红血球阳性急性淋巴菌白血病(Ph+AL)进行了调查. 甲状体盐形式可以提高溶性性和生物利用率,改善药用植物动力特性. 临床和临床研究表明,对抗耐药性突变的病人可以采取有力的抑制性活动,为抗病或复发性疾病患者提供治疗选择. 其选择性的,有约束力和有利的安全性特征进一步支持其精密的肿瘤应用潜力.
- 英文名称3-((1H-Pyrazolo[3,4-B]Pyridin-5-yl)Ethynyl)-4-Methyl-N-(4-((4-Methylpiperazin-1-yl)Methyl)-3-(Trifluoromethyl)Phenyl)Benzamide Dimethanesulfonate
- 中文名称GZD824甲磺酸盐
- IUPAC名称3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate
- 其它别名Levighxvovrogw-Uhfffaoysa-N; 4-Methyl-N-[4-[(4-Methylpiperazin-1-yl)Methyl]-3-(Trifluoromethyl)Phenyl]-3-[2-(1H-Pyrazolo[3,4-B]Pyrid
- CAS编号1421783-64-3
- MFCD编号:MFCD26142656
- FDA UNII编号:NPJ9AW8AZR
- 分子式:C31H35F3N6O7S2分子量:724.78
- 产品CID: 646238
- 同类组份化合物CAS1257628-77-5 (free base)1421783-64-3 (dimesylate)
- 产品分类生物化工 → 抑制剂 → 血管生成(Angiogenesis)
物理性质
- PSA:139.9
- LogP:5.2182
- 溶解性≥36.25 mg/mL In DMSO; ≥33.95 mg/mL In H2O With Ultrasonic; ≥4.71 mg/mL In Etoh With Ultrasonic
- 外观形态淡黄色至黄色固体
- 储存条件4°C, 防潮和避光
- 产品应用该化合物用作治疗慢性流星白血病(CML)和其他BCRE-AL驱动恶性肿瘤,特别是存放T315I变异或其他抗性相关BCR-ABL变异的恶性恶性病毒;它有效抑制了BF3细胞中表达野型BCR-ABL或BCL(T3150I)的BCRKL和STA5的BRKL及其下游效应器的活化,并在K562和KU812基因变异模型中以及在表达BCRO-AGL(WT)或BCRC-A BL(T315 I)的ALOGRAFT模型中展示了强大的抗瘤活动.
上下游产品
3-iodo-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl) phenyl)benzamide 5-ethynyl-1H-pyrazolo[3,4-b]pyridine methanesulfonic acid 3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide合成工艺路线路线简述
📜4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-B]吡啶-5-基)乙炔基]苯甲酰胺 以97的收率获得gzd824甲磺酸盐
参考文献:J. Med. Chem. 2013,56,879-894
标题:J. Med. Chem. 2013,56,879-894
海关参考信息
- 2901292000-乙炔
2912110000-甲醛
2912210000-苯甲醛
2921211000-乙二胺 - 💡 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
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📌 第三方产品分析报告
主要参考文献
1: Tang H, Jia W, Jia S, Dong R, Gao S, Feng J, Dong H, Gu H, Zhang T, Yuan R, Liu X, Cheng L, Zhou S, Gao G. A new chemotherapy-free regimen of olverembatinib in combination with venetoclax and dexamethasone for newly diagnosed Ph+ acute lymphoblastic leukemia: Preliminary outcomes of a prospective study. Am J Hematol. 2024 Mar 14. doi: 10.1002/ajh.27289. Epub ahead of print. 10(1):10. doi: 10.1038/s41421-023-00639-8. Erratum in: Cell Discov. 2024 Feb 26;10(1):23.
3: Sanz Murillo M, Villagran Suarez A, Dederer V, Chatterjee D, Alegrio Louro J, Knapp S, Mathea S, Leschziner AE. Inhibition of Parkinson's disease-related LRRK2 by type I and type II kinase inhibitors: Activity and structures. Sci Adv. 2023 Dec;9(48):eadk6191. doi: 10.1126/sciadv.adk6191. Epub 2023 Dec 1.
4: Ding J, Li W. Case report: Olverembatinib monotherapy: the chemotherapy-free regimen for an elderly patient with relapsed Ph-positive acute lymphoblastic leukemia. Front Pharmacol. 2023 Nov 16;14:1320641. doi: 10.3389/fphar.2023.1320641.
合成参考文献
参考文献:10.1016/j.bmc.2023.117561
摘要:Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM. Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors. Bioorg Med Chem. 2024 Jan 15;98():117561. doi: 10.1016/j.bmc.2023.117561.
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