MK-0752 化学構造
分子量: 442.9



Quality Control & MSDS


  • Compare Gamma-secretase Inhibitors
  • 研究分野



情報 MK-0752は適度に強力なγ-秘密アーゼ阻害剤です。そして、それは人間のSH-SY5Y独房で5nMのIC50でAβ40生産を減らします。
目標 γ-secretase
IC50 5 nM [1]
In vitro試験 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. [1] In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. [2]
In vivo試験 MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. [1] In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2]
臨床試験 MK-0752 study has been completed in Phase I clinical trials in patients with Metastatic or Locally Advanced Breast Cancer and Other Solid Tumors.
特集 A moderately potent γ-secretase inhibitor.

推薦された実験操作 (公開の文献だけ)

動物実験: [1]

動物モデル Cisterna Magna Ported (CMP) Rhesus Monkey Model.
製剤 MK-0752 is dissolved in water.
投薬量 ≤240 mg/kg
管理 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download MK-0752 SDF
分子量 442.9


CAS No. 471905-41-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 89 mg/mL (200.94 mM)
エタノール 45 mg/mL (101.6 mM)
<1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid

カスタマーレビュー (1)

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Source Oncotarget, 2014, 5(2), 363-74. MK-0752 purchased from Selleck
Method Cell viability assays
Cell Lines Hs683-Rl glioblastoma cells
Incubation Time
Results Subsequently, it assessed the inhibitory effects of the clinically available GSIs RO4929097, BMS-708163, LY450139, and MK-0752 on the Notch pathway by determining HES1 expression after GSI treatment.

製品表彰状 (1)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description