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RMC-6272

Catalog No. T39959   CAS 2382769-46-0
Synonyms: RM-006, RMC-6272

RMC-6272 (RM-006) is a bi-steric inhibitor that selectively targets mTORC1, displaying potent and selective (< 10-fold) inhibition over mTORC2. Compared to Rapamycin, RMC-6272 demonstrates enhanced inhibition of mTORC1 and induces increased cell death in TSC2 null tumors.

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RMC-6272 Chemical Structure
RMC-6272, CAS 2382769-46-0
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RMC-6272 (RM-006) is a bi-steric inhibitor that selectively targets mTORC1, displaying potent and selective (> 10-fold) inhibition over mTORC2. Compared to Rapamycin, RMC-6272 demonstrates enhanced inhibition of mTORC1 and induces increased cell death in TSC2 null tumors.
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-BP1 T37/46 , while inhibition of pS6 S240/244 levels is similar for Rapamycin and RM compounds[1].
In vivo RMC-6272 significantly decreases the kidney tumor burden in Tsc2 +/- A/J mice within four weeks of treatment. When assessed two months post-treatment cessation, the tumor burden remains notably lower in the RMC-6272 group compared to both the Rapamycin and MLN0128 groups[1].
Synonyms RM-006, RMC-6272
Molecular Weight 1850.25
Formula C95H141FN6O27S
CAS No. 2382769-46-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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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Keywords

RMC-6272 2382769-46-0 RM 006 RM-006 RM006 RMC 6272 RMC6272 inhibitor inhibit

 

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