RMC-6272 (Synonyms: RM-006) |
| Catalog No.GC63894 |
RMC-6272 (RM-006) est un inhibiteur sélectif bi-stérique de mTORC1. RMC-6272 présente une inhibition puissante et sélective (> 10 fois) de mTORC1 par rapport À mTORC2. Le RMC-6272 montre une meilleure inhibition de mTORC1 par rapport À la rapamycine et induit plus de mort cellulaire dans les tumeurs nulles TSC2.
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Cas No.: 2382769-46-0
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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].
[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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