630100-90-2
Chemical Structure
E7107
- CAS No.: 630100-90-2
- Formula:C40H66N2O9
- Molecular Weight:718.97
IUPAC Name: (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-2-((R,2E,4E)-6-hydroxy-7-((2R,3R)-3-((2R,3S)-3-hydroxypentan-2-yl)oxiran-2-yl)-6-methylhepta-2,4-dien-2-yl)-3,7-dimethyl-12-oxooxacyclododec-4-en-6-yl 4-cycloheptylpiperazine-1-carboxylate
InChIKey: MNOMBFWMICHMKG-MGYWSNOQSA-N
SMILES: [C@H]([C@H](CC)O)(C)[C@@]1([C@@H](C[C@@](/C=C/C=C(\C)/[C@@H]2[C@@H](C)/C=C/[C@H](OC(=O)N3CCN(CC3)C4CCCCCC4)[C@](C)(O)CC[C@@H](O)CC(=O)O2)(C)O)O1)[H]
Biological Activity: E7107 is a pre-mRNA spliceosome inhibitor and apoptosis (Apoptosis) inducer. E7107 binds to spliceosome-associated protein 130, inhibits spliceosome assembly and pre-mRNA splicing, regulates cellular protein expression, induces G1 and G2/M phase cell cycle arrest, triggers DNA damage, alters R-loop levels, reduces CHEK2 expression, impairs transcriptional elongation, and shifts MCL1 splicing toward pro-apoptotic isoforms. E7107 inhibits tumor growth in xenograft models and reduces leukemia burden. E7107 can be used in the research of advanced solid tumors, acute myeloid leukemia, T-cell acute lymphoblastic leukemia, and triple-negative breast cancer[1][2][3][4].
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E7107 | E7107 is a pre-mRNA spliceosome inhibitor and apoptosis (Apoptosis) inducer. E7107 binds to spliceosome-associated protein 130, inhibits spliceosome assembly and pre-mRNA splicing, regulates cellular protein expression, induces G1 and G2/M phase cell cycle arrest, triggers DNA damage, alters R-loop levels, reduces CHEK2 expression, impairs transcriptional elongation, and shifts MCL1 splicing toward pro-apoptotic isoforms. E7107 inhibits tumor growth in xenograft models and reduces leukemia burden. E7107 can be used in the research of advanced solid tumors, acute myeloid leukemia, T-cell acute lymphoblastic leukemia, and triple-negative breast cancer. | |||||||||||||||||||||
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References
- [1]. Hong DS, et al. A phase I, open-label, single-arm, dose-escalation study of E7107, a precursor messenger ribonucleic acid (pre-mRNA) splicesome inhibitor administered intravenously on days 1 and 8 every 21 days to patients with solid tumors. Investigational new drugs. 2014 Jun;32(3):436-44.
- [2]. Lee SC, et al. Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins. Nat Med. 2016 Jun;22(6):672-8. doi: 10.1038/nm.4097. Epub 2016 May 2. Erratum in: Nat Med. 2016 Jun 7;22(6):692.
- [3]. Han C, et al. SF3B1 homeostasis is critical for survival and therapeutic response in T cell leukemia. Science advances. 2022 Jan 21;8(3):eabj8357. [Content Brief]
- [4]. Chan S, et al. Basal-A Triple-Negative Breast Cancer Cells Selectively Rely on RNA Splicing for Survival. Molecular cancer therapeutics. 2017 Dec;16(12):2849-2861.
