MK-0752 - CAS 471905-41-6
Catalog number: 471905-41-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H21ClF2O4S
Molecular Weight:
442.9
COA:
Inquire
Targets:
γ-secretase
Description:
MK 0752, a potent, reversible inhibitor of γ-secretase (IC50 ~50 nM), reduces the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells (IC50= 5 nM).
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Brife Description:
A potent, reversible inhibitor of γ-secretase
Appearance:
White to off-white solid
Synonyms:
3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid; 3-(4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid; MK 0752; MK-0752; MK0752; 471905-41-6
Solubility:
Soluble to >10 mM in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -42℃ for long term (months to years).
MSDS:
Inquire
InChIKey:
XCGJIFAKUZNNOR-UHFFFAOYSA-N
InChI:
1S/C21H21ClF2O4S/c22-15-2-5-17(6-3-15)29(27,28)21(18-13-16(23)4-7-19(18)24)11-9-14(10-12-21)1-8-20(25)26/h2-7,13-14H,1,8-12H2,(H,25,26)
Canonical SMILES:
C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
1.Results of a phase 1 trial combining ridaforolimus and MK-0752 in patients with advanced solid tumours.
Piha-Paul SA1, Munster PN2, Hollebecque A3, Argilés G4, Dajani O5, Cheng JD6, Wang R6, Swift A6, Tosolini A6, Gupta S7. Eur J Cancer. 2015 Sep;51(14):1865-73. doi: 10.1016/j.ejca.2015.06.115. Epub 2015 Jul 18.
BACKGROUND: The phosphatidylinositol 3-kinase/protein kinase-B/mammalian target of rapamycin (PI3K-AKT-mTOR) signalling pathway is aberrantly activated in several cancers. Notch signalling maintains cell proliferation, growth and metabolism in part by driving the PI3K pathway. Combining the mTOR inhibitor ridaforolimus with the Notch inhibitor MK-0752 may increase blockade of the PI3K pathway.
2.Phase I trial of weekly MK-0752 in children with refractory central nervous system malignancies: a pediatric brain tumor consortium study.
Hoffman LM1, Fouladi M, Olson J, Daryani VM, Stewart CF, Wetmore C, Kocak M, Onar-Thomas A, Wagner L, Gururangan S, Packer RJ, Blaney SM, Gajjar A, Kun LE, Boyett JM, Gilbertson RJ. Childs Nerv Syst. 2015 Aug;31(8):1283-9. doi: 10.1007/s00381-015-2725-3. Epub 2015 May 1.
PURPOSE: Amplification and high levels of NOTCH ligand expression have been identified in several types of pediatric brain tumors. A phase I trial of weekly MK-0752, an oral inhibitor of gamma-secretase, was conducted in children with recurrent central nervous system (CNS) malignancies to estimate the maximum tolerated dose, dose-limiting toxicities (DLT), pharmacokinetics (PK), and pharmacodynamics of weekly MK-0752.
3.A parallel-arm phase I trial of the humanised anti-IGF-1R antibody dalotuzumab in combination with the AKT inhibitor MK-2206, the mTOR inhibitor ridaforolimus, or the NOTCH inhibitor MK-0752, in patients with advanced solid tumours.
Brana I1, Berger R2, Golan T2, Haluska P3, Edenfield J4, Fiorica J5, Stephenson J4, Martin LP6, Westin S7, Hanjani P8, Jones MB9, Almhanna K10, Wenham RM10, Sullivan DM11, Dalton WS12, Gunchenko A9, Cheng JD9, Siu LL1, Gray JE10. Br J Cancer. 2014 Nov 11;111(10):1932-44. doi: 10.1038/bjc.2014.497. Epub 2014 Oct 7.
BACKGROUND: Two strategies to interrogate the insulin growth factor 1 receptor (IGF-1R) pathway were investigated: vertical inhibition with dalotuzumab and MK-2206 or ridaforolimus to potentiate PI3K pathway targeting and horizontal cross-talk inhibition with dalotuzumab and MK-0752 to exert effects against cellular proliferation, angiogenesis, and stem cell propagation.
4.Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752.
Chen X1, Gong L1, Ou R1, Zheng Z1, Chen J1, Xie F1, Huang X1, Qiu J2, Zhang W2, Jiang Q2, Yang Y2, Zhu H1, Shi Z3, Yan X4. Gynecol Oncol. 2016 Mar;140(3):537-44. doi: 10.1016/j.ygyno.2015.12.011. Epub 2015 Dec 15.
OBJECTIVE: Ovarian cancer is one of the most lethal of women cancers and lack potent therapeutic options. There have many evidences demonstrate the Notch signaling has deregulation in variety of human malignancies.MK-0752 is a novel potent γ-secretase inhibitor and now assessed in clinical trial for treatment of several types of cancer, our objective was to investigate the anticancer effects and mechanisms of MK-0752 alone or combined with cisplatin in ovarian cancer.
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Chemical Structure

CAS 471905-41-6 MK-0752

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