MK-0752 Sodium

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525671

CAS#: 656810-87-6

Description: MK-0752 Sodium 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.

Chemical Structure

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MK-0752 Sodium
CAS# 656810-87-6
Instruction

Theoretical Analysis

MedKoo Cat#: 525671
Name: MK-0752 Sodium
CAS#: 656810-87-6
Chemical Formula: C21H20ClF2NaO4S
Exact Mass: 464.06
Molecular Weight: 464.884
Elemental Analysis: C, 54.26; H, 4.34; Cl, 7.63; F, 8.17; Na, 4.95; O, 13.77; S, 6.90

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: MK0752; MK 0752; MK-0752

IUPAC/Chemical Name: sodium 3-(4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoate

InChi Key: WFPVQMLUYJLUCN-UHFFFAOYSA-M

InChi Code: InChI=1S/C21H21ClF2O4S.Na/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);/q;+1/p-1

SMILES Code: O=C([O-])CCC1CCC(C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1.[Na+]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 464.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: 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. Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752. Gynecol Oncol. 2016 Mar;140(3):537-44. doi: 10.1016/j.ygyno.2015.12.011. Epub 2015 Dec 15. PubMed PMID: 26704638.
2: Piha-Paul SA, Munster PN, Hollebecque A, Argilés G, Dajani O, Cheng JD, Wang R, Swift A, Tosolini A, Gupta S. Results of a phase 1 trial combining ridaforolimus and MK-0752 in patients with advanced solid tumours. Eur J Cancer. 2015 Sep;51(14):1865-73. doi: 10.1016/j.ejca.2015.06.115. Epub 2015 Jul 18. PubMed PMID: 26199039.
3: Hoffman LM, 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. Phase I trial of weekly MK-0752 in children with refractory central nervous system malignancies: a pediatric brain tumor consortium study. Childs Nerv Syst. 2015 Aug;31(8):1283-9. doi: 10.1007/s00381-015-2725-3. Epub 2015 May 1. PubMed PMID: 25930724; PubMed Central PMCID: PMC4681692.
4: Brana I, Berger R, Golan T, Haluska P, Edenfield J, Fiorica J, Stephenson J, Martin LP, Westin S, Hanjani P, Jones MB, Almhanna K, Wenham RM, Sullivan DM, Dalton WS, Gunchenko A, Cheng JD, Siu LL, Gray JE. 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. Br J Cancer. 2014 Nov 11;111(10):1932-44. doi: 10.1038/bjc.2014.497. Epub 2014 Oct 7. PubMed PMID: 25290091; PubMed Central PMCID: PMC4229637.
5: Krop I, Demuth T, Guthrie T, Wen PY, Mason WP, Chinnaiyan P, Butowski N, Groves MD, Kesari S, Freedman SJ, Blackman S, Watters J, Loboda A, Podtelezhnikov A, Lunceford J, Chen C, Giannotti M, Hing J, Beckman R, Lorusso P. Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors. J Clin Oncol. 2012 Jul 1;30(19):2307-13. doi: 10.1200/JCO.2011.39.1540. Epub 2012 Apr 30. PubMed PMID: 22547604.
6: Whitehead J, Thygesen H, Jaki T, Davies S, Halford S, Turner H, Cook N, Jodrell D. A novel Phase I/IIa design for early phase oncology studies and its application in the evaluation of MK-0752 in pancreatic cancer. Stat Med. 2012 Aug 15;31(18):1931-43. doi: 10.1002/sim.5331. Epub 2012 Apr 11. PubMed PMID: 22495759.
7: Fouladi M, Stewart CF, Olson J, Wagner LM, Onar-Thomas A, Kocak M, Packer RJ, Goldman S, Gururangan S, Gajjar A, Demuth T, Kun LE, Boyett JM, Gilbertson RJ. Phase I trial of MK-0752 in children with refractory CNS malignancies: a pediatric brain tumor consortium study. J Clin Oncol. 2011 Sep 10;29(26):3529-34. doi: 10.1200/JCO.2011.35.7806. Epub 2011 Aug 8. PubMed PMID: 21825264; PubMed Central PMCID: PMC3179253.
8: 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. doi: 10.1016/j.jchromb.2010.07.019. Epub 2010 Jul 30. Erratum in: J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Nov 1;908:161. PubMed PMID: 20702149; PubMed Central PMCID: PMC2926936.