MS023 dihydrochloride - CAS:1992047-64-9

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MS023 dihydrochloride

目录号 : KM11683 CAS No. : 1992047-64-9 纯度 : 98%

Data Sheet 产品使用指南

MS023 dihydrochloride 是一种有效选择性的，具有细胞活性的人 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，对 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC₅₀ 分别为 30，119，83，4 和 5 nM。

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生物活性

MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC₅₀s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

体外研究

MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells.
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells.

Western Blot Analysis

Cell Line:	MCF7 and HEK293 cells
Concentration:	1.4, 4, 12, 37, 111, 333, and 1000 nM
Incubation Time:	48 hours for MCF7 cells; 20 hours for HEK293 cells
Result:	Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC₅₀=9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC₅₀=56±7 nM).

体内研究

Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells.

Animal Model:	NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells
Dosage:	160 mg/kg
Administration:	Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result:	Combinatorial treatment extended survival of leukemic mice relative to single treatments.

分子式

C₁₇H₂₇Cl₂N₃O

分子量

360.32

CAS号

1992047-64-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (416.30 mM)

H₂O : 33.33 mg/mL (92.50 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7753 mL	13.8766 mL	27.7531 mL
5 mM	0.5551 mL	2.7753 mL	5.5506 mL
10 mM	0.2775 mL	1.3877 mL	2.7753 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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The molarity calculator equation

The dilution calculator equation