For research use only. Not for therapeutic Use.
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].
| Catalog Number | I044528 |
| CAS Number | 2382769-46-0 |
| Synonyms | [(1R,2R,4S)-2-methoxy-4-[(2R)-2-[(1R,9S,12S,14R,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,14,18-trihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,20-tetraoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]cyclohexyl] N-[2-[2-[2-[2-[2-[2-[2-[2-[3-[2-[4-[7-(6-aminopyridin-3-yl)-3,5-dihydro-2H-1,4-benzoxazepine-4-carbonyl]-2-fluoro-3-methylphenyl]sulfonylethylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]carbamate |
| Molecular Formula | C95H141FN6O27S |
| Purity | ≥95% |
| InChI | InChI=1S/C95H141FN6O27S/c1-62-17-13-12-14-18-63(2)80(115-9)58-74-24-20-68(7)95(112,129-74)90(107)92(109)102-33-16-15-19-76(102)93(110)127-81(59-77(103)64(3)54-67(6)88(106)89(117-11)87(105)66(5)53-62)65(4)55-70-21-26-79(82(56-70)116-10)128-94(111)99-31-36-119-39-41-121-43-45-123-47-49-125-51-50-124-48-46-122-44-42-120-40-38-118-35-30-85(104)98-32-52-130(113,114)83-28-25-75(69(8)86(83)96)91(108)101-34-37-126-78-27-22-71(57-73(78)61-101)72-23-29-84(97)100-60-72/h12-14,17-18,22-23,25,27-29,54,57,60,62,64-66,68,70,74,76-77,79-82,88-89,103,106,112H,15-16,19-21,24,26,30-53,55-56,58-59,61H2,1-11H3,(H2,97,100)(H,98,104)(H,99,111)/b14-12+,17-13+,63-18+,67-54+/t62-,64-,65-,66-,68-,70+,74+,76+,77-,79-,80+,81+,82-,88-,89+,95-/m1/s1 |
| InChIKey | SBCMKKFTXRBACH-URWOFZDBSA-N |
| SMILES | CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)NCCS(=O)(=O)C5=C(C(=C(C=C5)C(=O)N6CCOC7=C(C6)C=C(C=C7)C8=CN=C(C=C8)N)C)F)O)C)C)O)OC)C)C)C)OC |
| Reference | [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 |
