NPS-1034|cas:1221713-92-3|西域试剂

NPS-1034,98.0%

产品编号：Bellancom-100509| CAS NO：1221713-92-3| 分子式：C₃₁H₂₃F₂N₅O₃| 分子量：551.54

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-100509	￥990.00	杭州北京（现货）
Bellancom-100509	￥1550.00	杭州北京（现货）
Bellancom-100509	￥3100.00	杭州北京（现货）
Bellancom-100509	￥4950.00	杭州北京（现货）
Bellancom-100509	￥6800.00	杭州北京（现货）

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NPS-1034

产品介绍

NPS-1034 是 AXL 和 MET 的双重抑制剂，其 IC₅₀ 值分别为 10.3 和 48 nM。

生物活性

NPS-1034 is a dual inhibitor of AXL and MET with IC₅₀s of 10.3 and 48 nM, respectively.

体外研究

NPS-1034 is a dual inhibitor of AXL and MET with IC₅₀s of 10.3 and 48 nM, respectively.The expression and activity of AXL is significantly increased in HCC827/ER cells, and NPS-1034 treatment effectively inhibits its tyrosine phosphorylation. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC₅₀ values of 112.7 and 190.3 nmol, respectively. In contrast, NPS-1034 inhibits AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell viability with IC₅₀ values ranging from 1 μmol to more than 10 μmol. MET phosphorylation is dramatically decreased after treatment with NPS-1034 in the MKN45 cells, but not in the MKN28 cells. NPS-1034 inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC₅₀ values of <10 and <50 nmol, respectively. HGF-induced MET phosphorylation is completely inhibited by 50 nmol NPS-1034.

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

体内研究

NPS-1034 inhibits tumor proliferation, which highly expresses p-MET. NPS-1034 treatment induces a clear decrease in the vascularization of the tumors. The expression of alpha-smooth muscle actin (α-SMA) is decreased in the tumor sections of mice treated with NPS-1034. NPS-1034-treated mice show virtually no weight loss, indicating that NPS-1034 is generally well tolerated.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 34 mg/mL (61.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8131 mL	9.0655 mL	18.1311 mL
5 mM	0.3626 mL	1.8131 mL	3.6262 mL
10 mM	0.1813 mL	0.9066 mL	1.8131 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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式