2250059-80-2
Chemical Structure
RMC-4745
- CAS No.: 2250059-80-2
- Formula:C94H142N12O24
- Molecular Weight:1824.20
IUPAC Name: (9Z,12Z)-octadeca-9,12-dien-1-yl ((((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)-L-alaninate
InChIKey: LRYDUVDTGSMHSI-CKZJDGLRSA-N
SMILES: NC1=C2C(C3=CC4=CC(O)=CC=C4N3)=NN(C2=NC=N1)CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCN5C=C(N=N5)CCCCO[C@H]6[C@@H](C[C@@H](CC6)C[C@H]([C@@]7([H])OC([C@@]8([H])N(CCCC8)C(C([C@@]9(O[C@](CC[C@H]9C)([H])C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@H](C([C@@H]([C@@H](/C(C)=C/[C@H](C(C7)=O)C)O)OC)=O)C)C)NC(OC)=O)O)=O)=O)=O)C)OC)=O
Biological Activity: RMC-4745 is a selective dual-site inhibitor of mTORC1, with a selectivity of 35 times for mTORC1 and mTORC2. RMC-4745 inhibits the proliferation of MCF-7 cells and upregulates Caspase-3/7 activity to induce cell apoptosis. RMC-4745 does not cause the upregulation of HER3 due to the inhibition of mTORC2. RMC-4745 can be used for the study of breast cancer[1].
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RMC-4745 | RMC-4745 is a selective dual-site inhibitor of mTORC1, with a selectivity of 35 times for mTORC1 and mTORC2. RMC-4745 inhibits the proliferation of MCF-7 cells and upregulates Caspase-3/7 activity to induce cell apoptosis. RMC-4745 does not cause the upregulation of HER3 due to the inhibition of mTORC2. RMC-4745 can be used for the study of breast cancer. | |||||||||||||||||||||
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References
- [1]. Lee BJ, et al. Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth. Nat Chem Biol. 2021 Oct;17(10):1065-1074. doi: 10.1038/s41589-021-00813-7. Epub 2021 Jun 24. Erratum in: Nat Chem Biol. 2021 Aug;17(8):925. doi: 10.1038/s41589-021-00843-1. Erratum in: Nat Chem Biol. 2021 Nov;17(11):1209. [Content Brief]
