623165-93-5
Chemical Structure
MRK 003
- CAS No.: 623165-93-5
- Formula:C25H31F6N3O2S
- Molecular Weight:551.59
IUPAC Name: (3R,6'S,9'R)-5-(2,2,2-trifluoroethyl)-2'-((E)-3-(4-(trifluoromethyl)piperidin-1-yl)prop-1-en-1-yl)-5',6',7',8',9',10'-hexahydrospiro[[1,2,5]thiadiazolidine-3,11'-[6,9]methanobenzo[8]annulene] 1,1-dioxide
InChIKey: NKHUILHBYOOZDF-NCOIWELASA-N
SMILES: FC(F)(F)CN(C[C@]1(N2)[C@H]3CC4=C(C=CC(/C=C/CN5CCC(C(F)(F)F)CC5)=C4)C[C@@H]1CC3)S2(=O)=O
Biological Activity: MRK 003 is an orally active γ-secretase inhibitor. MRK 003 targets the Notch signaling pathway by blocking the proteolytic cleavage of Notch receptors. MRK 003 inhibits tumor cell proliferation, induces apoptosis, downregulates anti-apoptotic proteins, upregulates phosphorylated Akt, suppresses angiogenesis, and overcomes microenvironment-mediated proliferative protection. MRK 003 can be used in research related to lung cancer, multiple myeloma, non-Hodgkin's lymphoma, pancreatic ductal adenocarcinoma, glioblastoma, and breast cancer[1][2][3][4][5][6][7].
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MRK 003 | MRK 003 is an orally active γ-secretase inhibitor. MRK 003 targets the Notch signaling pathway by blocking the proteolytic cleavage of Notch receptors. MRK 003 inhibits tumor cell proliferation, induces apoptosis, downregulates anti-apoptotic proteins, upregulates phosphorylated Akt, suppresses angiogenesis, and overcomes microenvironment-mediated proliferative protection. MRK 003 can be used in research related to lung cancer, multiple myeloma, non-Hodgkin's lymphoma, pancreatic ductal adenocarcinoma, glioblastoma, and breast cancer. | |||||||||||||||||||||
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References
- [1]. Konishi J, et al. Gamma-secretase inhibitor prevents Notch3 activation and reduces proliferation in human lung cancers. Cancer research. 2007 Sep 01;67(17):8051-7. [Content Brief]
- [2]. Watters JW et al. De novo discovery of a gamma-secretase inhibitor response signature using a novel in vivo breast tumor model. Cancer Res. 2009 Dec 1;69(23):8949-8957. [Content Brief]
- [3]. Pandya K, et al. Targeting both Notch and ErbB-2 signalling pathways is required for prevention of ErbB-2-positive breast tumour recurrence. British journal of cancer. 2011 Sep 06;105(6):796-806. [Content Brief]
- [4]. Ramakrishnan V, et al. MRK003, a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. Leukemia. 2012 Feb;26(2):340-8. [Content Brief]
- [5]. Kondratyev M, et al. Gamma-secretase inhibitors target tumor-initiating cells in a mouse model of ERBB2 breast cancer. Oncogene. 2012 Jan 05;31(1):93-103. [Content Brief]
- [6]. Mizuma M, et al. The gamma secretase inhibitor MRK-003 attenuates pancreatic cancer growth in preclinical models. Molecular cancer therapeutics. 2012 Sep;11(9):1999-2009. [Content Brief]
- [7]. Chu Q, et al. Prolonged inhibition of glioblastoma xenograft initiation and clonogenic growth following in vivo Notch blockade. Clinical cancer research : an official journal of the American Association for Cancer Research. 2013 Jun 15;19(12):3224-33. [Content Brief]
