MS432|cas:2672512-44-4|西域试剂

MS432,98.20%

产品编号：Bellancom-130602| CAS NO：2672512-44-4| 分子式：C₅₀H₆₅F₃IN₇O₆S| 分子量：1076.06

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-130602		￥7000.00	杭州北京（现货）
Bellancom-130602		￥11500.00	杭州北京（现货）

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MS432

产品介绍

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。

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.

体外研究

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).

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

Cell Viability Assay

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.

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

Animal Model:	Male Swiss Albino mice.
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.

体内研究

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.

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

Animal Model:	Male Swiss Albino mice.
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.

体内研究

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.

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

Animal Model:	Male Swiss Albino mice.
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.

性状

Solid

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。