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NPS-1034 {[allProObj[0].p_purity_real_show]}

货号：A518169 Ambeed 开学季，买赠积分，赢豪礼

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

NPS-1034 化学结构 CAS号：1221713-92-3
NPS-1034 化学结构
CAS号：1221713-92-3
NPS-1034 3D分子结构
CAS号：1221713-92-3
NPS-1034 化学结构 CAS号：1221713-92-3
NPS-1034 3D分子结构 CAS号：1221713-92-3
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NPS-1034 纯度/质量文件 产品仅供科研

货号：A518169 标准纯度： {[allProObj[0].p_purity_real_show]}
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NPS-1034 生物活性

描述 NPS-1034 serves as a dual antagonist for AXL and MET, exhibiting IC50 values of 10.3 nM for AXL and 48 nM for MET. In HCC827/ER cells, where AXL's expression and activity are notably heightened, treatment with NPS-1034 successfully curtails its tyrosine phosphorylation. NPS-1034 reduces the viability of MKN45 and SNU638 cell lines, which have high expression levels of the MET gene and phosphorylated MET, with IC50 values of 112.7 nM and 190.3 nM, respectively. Conversely, it inhibits the viability of AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell lines with IC50 values ranging from 1 μM to over 10 μM. Treatment with NPS-1034 significantly lowers MET phosphorylation in MKN45 cells, but not in MKN28 cells. It also inhibits HGF-induced MET autophosphorylation in AGS and MKN1 cell lines with IC50 values of less than 10 nM and less than 50 nM, respectively, with 50 nM of NPS-1034 completely blocking HGF-induced MET phosphorylation[1].

NPS-1034 动物研究

Animal study NPS-1034 suppresses tumor growth in tumors that express high levels of phosphorylated MET and leads to a notable reduction in tumor vascularization. The expression of α-SMA is also reduced in the tumor sections of mice treated with NPS-1034. Mice treated with NPS-1034 exhibit no significant weight loss, suggesting that the compound is generally well-tolerated[2].

NPS-1034 参考文献

[1]Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.

[2]Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99.

NPS-1034 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.07mL

1.81mL

0.91mL

18.13mL

3.63mL

1.81mL

NPS-1034 技术信息

CAS号1221713-92-3
分子式C31H23F2N5O3
分子量 551.543
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 35 mg/mL(63.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: NPS-1034 | 1221713-92-3 | NPS1034 | NPS 1034 | AXL/MET Inhibitor | Protein Tyrosine Kinase/RTK | Apoptosis | TAM Receptor | c-Met/HGFR | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | NPS-1034 纯度/质量文件 | NPS-1034 生物活性 | NPS-1034 动物研究 | NPS-1034 参考文献 | NPS-1034 实验方案 | NPS-1034 技术信息

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