Rineterkib hydrochloride
目录号: PL10789 纯度: ≥99%
CAS No. :1715025-34-5
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中文名称
Rineterkib hydrochloride
英文名称
Rineterkib hydrochloride
英文别名
Rineterkib hydrochloride;8RS453RBHM;4-[3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]pyrazin-2-yl]-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluorobenzamide;hydrochloride;Benzamide, 4-(3-amino-6-((1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl)-2-pyrazinyl)-N-((1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl)-2-fluoro-, hydrochloride;Unii-8RS453rbhm
Cas No.
1715025-34-5
分子式
C26H28BrClF3N5O2
分子量
614.89
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
Rineterkib hydrochloride (compound B) 是具有口服活性的 ERK1 和ERK2 的抑制剂,通过激活 MAPK 通路中的突变来发挥抗增生作用。这种活性与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌以及 KRAS 突变型卵巢癌尤为相关。Rineterkib hydrochloride 也能抑制 RAF。
生物活性
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.
性状
Solid
体内研究(In Vivo)
ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
ClinicalTrial
参考文献
[1]. CAPONIGRO, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO2018051306A1.
[2]. Song Y, et al. Targeting RAS-RAF-MEK-ERK signaling pathway in human cancer: current status in clinical trials. Genes & Diseases, 2022.
溶解度数据
In Vitro: DMSO : 220 mg/mL (Need ultrasonic)In Vivo:请根据您的实验动物和给药
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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