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MK-0752 (471905-41-6)

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2….

Not Intended for Therapeutic Use. For research use only.

CAS: 471905-41-6 Category

MK-0752 (471905-41-6) Description:

MK0752 is a synthetic small molecule with potential antineoplastic activity. MK0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. The Notch signaling pathway plays an important role in cell-fate determination, cell survival, and cell proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells.  In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation.

MK-0752 (471905-41-6) Specifications:

Product Name MK-0752
Synonym MK0752; cis34(3chlorophenyl)sulfonyl4(25difluorophenyl)cyclohexyl propanoicacid.
Chemical Name 3-((1r,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid.
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 471905-41-6
Molecular Formula C21H21ClF2O4S
Molecular Weight 442.9
Monoisotopic Mass 442.08171 g/mol
MDL number MFCD16660191
InChIKey XCGJIFAKUZNNOR-HNSKJHPRSA-N
InChi Code 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)/t14-,21-
SMILES O=C(O)CC[[email protected]]1CC[[email protected]](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1
Form Solid powder
Color  
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >5 years if stored properly
Handling Protect from air and light
Application A moderately potent γ-secretase inhibitor.

 


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RIDADR NONH for all modes of transport

References:

[1]. Bai F, Tagen M, Colotta C, Miller L, Fouladi M, Stewart CF. Determination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52. Epub 2010 Jul 30. PubMed PMID: 20702149; PubMed Central PMCID: PMC2926936.

[2]. Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci. 2010 May 12;30(19):6743-50. PubMed PMID: 20463236; PubMed Central PMCID: PMC2913973.

[3]. Matthews CZ, Woolf EJ. Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Feb 15;863(1):36-45. Epub 2008 Jan 6. PubMed PMID: 18249589.

[4].Olson RE, Albright CF. Recent progress in the medicinal chemistry of gamma-secretase inhibitors. Curr Top Med Chem. 2008;8(1):17-33. Review. PubMed PMID: 18220929.

[5]. Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752. Chen X, Gong L, Ou R, Zheng Z, Chen J, Xie F, Huang X, Qiu J, Zhang W, Jiang Q, Yang Y, Zhu H, Shi Z, Yan X. Gynecol Oncol. 2016 Mar;140(3):537-44. doi: 10.1016/j.ygyno.2015.12.011. Epub 2015 Dec 15. PMID: 26704638.

1 review for MK-0752 (471905-41-6)

  1. Cofttek

    Never had such good experience before,The MK-0752 (471905-41-6) is high purity,also customer service is pretty nice !gotta try!!

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