MK-0752是一種有效的γ分泌酶抑制劑(IC50 ~50 nM)。γ分泌酶是NOTCH裂解機(jī)制中的一個重要成分，它催化受體蛋白底物在其跨膜結(jié)構(gòu)域內(nèi)的裂解。抑制Notch抑制BC細(xì)胞體外增殖。Notch信號需要γ分泌酶，γ分泌酶裂解Notch，釋放Notch胞內(nèi)結(jié)構(gòu)域(NICD)來激活靶基因的轉(zhuǎn)錄。NOTCH信號在正常組織發(fā)育、細(xì)胞命運決定、增殖和存活中起重要作用。NOTCH信號在包括Delta1、Delta2和Delta3以及Jagged1和Jagged2的同源配體結(jié)合后被激活。

產(chǎn)品性質(zhì)：

Cas No.：471905-41-6

別名：順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸,MK 0752, MK0752

化學(xué)名;3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid

Canonical SMILES:C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl

分子式:C21H21ClF2O4S

分子量：442.9

溶解度：≥ 22.15 mg/mL in DMSO, ≥ 48.8 mg/mL in EtOH with ultrasonic

儲存條件：Store at -20°C

注意事項：

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Reference：

[1].I. E. Krop, M. Kosh, I. Fearen, J. Savoie, A. Dallob, C. Matthews, J. Stone, E. Winer, S. J. Freedman and P. Lorusso. Phase I pharmacokinetic (PK), and pharmacodynamic (PD) trial of the novel oral Notch inhibitor MK-0752 in patients (pts) with advanced breast cancer (BC) and other solid tumors. J Clin Oncol (Meeting Abstracts) June 2006 vol. 24 no. 18_suppl 10574.

[2].Maryam Fouladi, Clinton F. Stewart, James Olson, Lars M. Wagner, Arzu Onar-Thomas, Mehmet Kocak, Roger J. Packer, Stewart Goldman, Sridharan Gururangan, Amar Gajjar, Tim Demuth, Larry E. Kun, James M. Boyett and Richard J. Gilbertson. Phase I Trial of MK-0752 in Children With Refractory CNS Malignancies: A Pediatric Brain Tumor Consortium Study. JCO September 10, 2011 vol. 29 no. 26 3529-3534