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.
性状
Solid
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-BP1, while inhibition of pS6 levels is similar for Rapamycin and RM compounds. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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 1
溶解度数据
In Vitro: DMSO : 25 mg/mL (13.51 mM; ultrasonic and warming and heat to 60°C)配制储备液