RMC-6272(Synonyms: RM-006)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RMC-6272 (Synonyms: RM-006)

RMC-6272 (RM-006) 是一种双空间的,选择性的 mTORC1 抑制剂,对 mTORC1 的抑制作用比 mTORC2 强且选择性 >10 倍。与雷帕霉素相比,RMC-6272 对 mTORC1 的抑制作用增强,并在 TSC2 阴性肿瘤中诱导更多的细胞死亡。

RMC-6272(Synonyms: RM-006)

RMC-6272 Chemical Structure

CAS No. : 2382769-46-0

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生物活性

RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors[1].

体外研究
(In Vitro)

RMC-6272 shows more effective growth inhibition in multiple TSC1 or TSC2 mutant tumor cell lines compared to Rapamycin. RMC-6272 causes a more profound growth inhibition in the TSC1 or TSC2 mutant cells than the wild type cells. RMC-6272 at ~1 nM shows near complete inhibition of p4E-BP1T37/46, while inhibition of pS6S240/244 levels is similar for Rapamycin and RM compounds[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RMC-6272 markedly reduces kidney tumor burden in Tsc2+/- A/J mice after four weeks of treatment. Tumor regrowth is assessed two months after treatment cessation, tumor burden is significantly reduced in the RMC-6272 group as compared to the Rapamycin and MLN0128 groups[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1850.22

Formula

C95H141FN6O27S

CAS 号

2382769-46-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Heng Du, et al. Bi-steric mTORC1-selective inhibitors demonstrate improved potency and efficacy in tumors with mTORC1 hyperactivation [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 1026.

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