M435-1279|cas:1359431-16-5|西域试剂

M435-1279,98.03%

产品编号：Bellancom-141891| CAS NO：1359431-16-5| 分子式：C₁₈H₁₇N₃O₅S₂| 分子量：419.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-141891	￥1500.00	杭州北京（现货）
Bellancom-141891	￥2500.00	杭州北京（现货）
Bellancom-141891	￥5500.00	杭州北京（现货）
Bellancom-141891	￥9500.00	杭州北京（现货）

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M435-1279

产品介绍

M435-1279 是 UBE2T 抑制剂。M435-1279 通过阻断 UBE2T 介导的 RACK1 降解来抑制 Wnt/β-catenin 信号通路的过度激活。

生物活性

M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.

体外研究

M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells.
M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability with IC₅₀s of 16.8, 11.88, 6.93, 7.76 μM of GES-1, HGC27, MKN45, AGS cells, respectively.
M435-1279 (31 nM to 500 μM) binds to UBE2T with a K_D value of 50.5 μM.
M435-1279 (11.88 μM; 48 h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway.

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

Cell Viability Assay

Cell Line:	HGC27, AGS, and MKN45 cells
Concentration:	0, 2, 4, 8, 16, 31 μM
Incubation Time:	48 h
Result:	Inhibited the cell growth.

Cell Viability Assay

Cell Line:	HGC27, AGS, and MKN45 cells
Concentration:	0, 4, 8, 12, 16, 20 μM
Incubation Time:
Result:	Inhibited the cell viability with IC₅₀s of 16.8, 11.88, 6.93, 7.76 μM in GES-1, HGC27, MKN45, AGS cells, respectively.

体内研究
(In Vivo)

M435-1279 (5 mg/kg/day; intratumor injection for 18 days) slows the tumor growth.
M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.

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

Animal Model:	BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm³)
Dosage:	5 mg/kg/day
Administration:	Intratumor injection for 18 days
Result:	Slowed the tumor growth. Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.

体内研究

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

Animal Model:	BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm³)
Dosage:	5 mg/kg/day
Administration:	Intratumor injection for 18 days
Result:	Slowed the tumor growth. Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.

体内研究

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

Animal Model:	BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm³)
Dosage:	5 mg/kg/day
Administration:	Intratumor injection for 18 days
Result:	Slowed the tumor growth. Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (119.20 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3840 mL	11.9198 mL	23.8396 mL
5 mM	0.4768 mL	2.3840 mL	4.7679 mL
10 mM	0.2384 mL	1.1920 mL	2.3840 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)。-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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明