MS432

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MS432  纯度: 98.20%

MS432 是创新的、高度选择性的、基于 PD0325901 和 von Hippel-Lindau 配体的 MEK1 和 MEK2 的 PROTAC 降解剂。MS432 在小鼠体内显示了较高且长时间的血浆暴露量，对 HT29 细胞中 MEK1 和 MEK2 蛋白的DC50 值分别为 31 nM 和 17 nM。

MS432

MS432 Chemical Structure

CAS No. : 2672512-44-4

规格 价格 是否有货 数量
5 mg ￥7000 In-stock
10 mg ￥11500 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively[1].

IC50 & Target[1]

MEK1

31 nM (DC50, in HT29 cells)

MEK2

17 nM (DC50, in HT29 cells)

MEK1

31 nM (DC50, in SK-MEL-28 cells)

MEK2

9.3 nM (DC50, in SK-MEL-28 cells)

体外研究
(In Vitro)

MS432 (compound 23) is potent in reducing MEK1/2 protein levels in COLO 205 cells (DC50 (MEK1) = 18 ± 7 nM, DC50 (MEK2) = 11 ± 2 nM) and UACC257 cells (DC50 (MEK1) = 56 ± 25 nM, DC50 (MEK2) = 27 ± 19 nM).

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: (HT-29, SK-MEL-28, COLO 205 and UACC 257 cell lines.
Concentration: 0-1 μM.
Incubation Time: 72 hours.
Result: Effectively inhibited proliferation of these CRC and melanoma cells in a concentration-dependent manner, with GI50 values ranging from 30 to 200 nM.

体内研究
(In Vivo)

MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI50 values of compound 23 in the tested cancer cell lines[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Swiss Albino mice[1].
Dosage: 50 mg/kg (Pharmacokinetic Analysis).
Administration: IP
Result: Displays good plasma exposure with the maximum plasma concentration of 1,400 nM detected at 0.5 hour post dosing and plasma concentration of 710 nM at 8 hours post dosing.

分子量

1076.06

Formula

C50H65F3IN7O6S
CAS 号

2672512-44-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 260 mg/mL (241.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9293 mL 4.6466 mL 9.2932 mL
5 mM 0.1859 mL 0.9293 mL 1.8586 mL
10 mM 0.0929 mL 0.4647 mL 0.9293 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 (protect from light, 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 6.5 mg/mL (6.04 mM); Clear solution

    此方案可获得 ≥ 6.5 mg/mL (6.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 65.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911.

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