MK-0752 化学構造
分子量: 442.9

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Quality Control & MSDS

製品説明

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    Gamma-secretase製品生物活性の比較
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製品の説明

生物活性

製品説明 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。
ターゲット 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.

プロトコル (参考用のみ)

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
投与方法 Administered via p.o.

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
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)
1

参考

化学情報

Download MK-0752 SDF
分子量 442.9
化学式

C21H21ClF2O4S

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

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Rating
Source Oncotarget, 2014, 5(2), 363-74. MK-0752 purchased from Selleck
Method Cell viability assays
Cell Lines Hs683-Rl glioblastoma cells
Concentrations
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.

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技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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