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MK-0752

Cat. No. M2120
MK-0752 Structure
Size Price Availability Quantity
10mg USD 245 In stock
50mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MK-0752 is a potent gamma secretase inhibitor, an enzyme required for Notch pathway activation. MK-0752 reduces Aβ40 production with IC50 of 5 nM in human SH-SY5Y cells. MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation in vitro. MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15 and Aβ 1-16, while decreases levels of Aβ 1-17. Phase I clinical trials has been completed in 2006, and the results reported showed that MK-0752 was well-tolerated in a limited number of patients below 300 mg/m2, and further enrollment was underway to establish the MTD.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 442.9
Formula C21H21ClF2O4S
CAS Number 471905-41-6
Purity >99%
Solubility DMSO 80 mg/mL
Ethanol 40 mg/mL
Storage at -20°C
References

Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors.
Krop I, et al. J Clin Oncol. 2012 Jul 1;30(19):2307-13. PMID: 22547604.

Phase I trial of MK-0752 in children with refractory CNS malignancies: a pediatric brain tumor consortium study.
Fouladi M, et al. J Clin Oncol. 2011 Sep 10;29(26):3529-34. PMID: 21825264.

Regulation of breast cancer stem cell activity by signaling through the Notch4 receptor.
Harrison H, et al. Cancer Res. 2010 Jan 15;70(2):709-18. PMID: 20068161.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-0752 supplier, Gamma-secretase, inhibitors

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