2382769-46-0

2382769-46-0 structure

Name: RMC-6272
Chemical Name: RMC-6272
CAS Number: 2382769-46-0
Molecular Formula: C₉₅H₁₄₁FN₆O₂₇S
Molecular Weight: 1850.22
Catalog: Signaling Pathways PI3K/Akt/mTOR mTOR
Create Date: 2021-12-19 21:15:29
Modify Date: 2024-01-09 20:54:48
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].

Name	RMC-6272

Description	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].
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> mTOR Research Areas >> Cancer
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].
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].
References	[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.

Molecular Formula	C₉₅H₁₄₁FN₆O₂₇S
Molecular Weight	1850.22