MRK 560|677772-84-8|-陌孚医药/Medlife

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MRK 560

目录号: PC15678 纯度: ≥98%

CAS No. :677772-84-8

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中文名称

MRK 560

中文别名

N-[顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己基]-1,1,1-三氟甲烷磺酰胺

英文名称

MRK 560

英文别名

Methanesulfonamide,N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoro-;MRK 560;N-{cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohe xyl}-1,1,1-trifluoromethanesulfonamide;MRK-560

Cas No.

677772-84-8

分子式

C₁₉H₁₇ClF₅NO₄S₂

分子量

517.92

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimers disease and T-cell acute lymphoblastic leukaemia (T-ALL).

性状

Solid

IC50 & Target[1][2]

PSEN1

体外研究(In Vitro)

MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	HPB-ALL, DND-41, and Jurkat cells
Concentration:	30, 100, 300, 1000 nM
Incubation Time:	15 days
Result:	Reduced NICD1 generation in cells and resulted in a dose-dependent decrease of proliferation in HPB-ALL and DND-41, which depend on NOTCH signaling for their survival.

体内研究(In Vivo)

MRK-560 (15.54 mg/kg; S.C.; single daily for 14 days) shows strong antileukemic effects on T-ALL model.
MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) shows good blood-brain barrier permeability in a dose-dependent manner in rats.

MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) inhibits the production of Aβ levels in brain and cerebrospinal fluid.
MRK-560 (1 mg/kg; p.o.; single) shows a good bioavailability of 70 to 90%, and T_max is 12 h.
MRK-560 (1 mg/kg; i.v.; single) is suitable for once-a-day dosing (with a low plasma clearance and a half-life of more than 15 h).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:	15.54 mg/kg
Administration:	Subcutaneous injection; single daily for 14 days.
Result:	Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1, 3, 10, 30, 100 mg/kg
Administration:	Oral administration; single (experiment is performed 8 h later)
Result:	Increased the plasma and brain concentrations in a dose-dependent manner. Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1 mg/kg
Administration:	Intravenously and orally administration; single.
Result:	Showed T_max after the oral dose was 12 h,and bioavailability was 70 to 90%. Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Habets RA, et al. Safe targeting of T cell acute lymphoblastic leukemia by pathology-specific NOTCH inhibition. Sci Transl Med. 2019 May 29;11(494):eaau6246. [Information]

[2]. Best JD, et al. In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in t

溶解度数据

体外研究:

DMSO : 100 mg/mL (193.08 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9308 mL	9.6540 mL	19.3080 mL
5 mM	0.3862 mL	1.9308 mL	3.8616 mL
10 mM	0.1931 mL	0.9654 mL	1.9308 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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