1. Protein Tyrosine Kinase/RTK Apoptosis
  2. TAM Receptor c-Met/HGFR Apoptosis
  3. NPS-1034

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

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NPS-1034 Chemical Structure

NPS-1034 Chemical Structure

CAS No. : 1221713-92-3

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10 mM * 1 mL in DMSO ¥1068
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5 mg ¥880
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10 mg ¥1320
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25 mg ¥2420
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50 mg ¥3630
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100 mg ¥5390
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

IC50: 10.3 nM (AXL), 48 nM (MET)[1]

体外研究
(In Vitro)

NPS-1034 是 AXL 和 MET 的双重抑制剂,IC50 分别为 10.3 和 48 nM。AXL 的表达和活性在 HCC827/ER 细胞中显著增加,NPS-1034 处理有效抑制其酪氨酸磷酸化[1]。NPS-1034 抑制高度表达 MET 基因和 p-MET (磷酸化 MET) 的 MKN45 和 SNU638 细胞系的活力,IC50 值分别为 112.7 和 190.3 nMol。相反,NPS-1034 抑制 AGS、KATOIII、NCI-N87、MKN1、MKN28 和 MKN74 细胞活力,IC50 值范围为 1 μMol 至超过 10 μMol。在 MKN45 细胞中用 NPS-1034 处理后 MET 磷酸化显著降低,但在 MKN28 细胞中没有。NPS-1034 在 AGS 和 MKN1 细胞系中抑制肝细胞生长因子 (HGF) 刺激的 MET 自磷酸化 (Y1234/1235),IC50 值分别为 <10 和 <50 nMol。HGF 诱导的 MET 磷酸化被 50 nMol NPS-1034 完全抑制[2]

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

体内研究
(In Vivo)

NPS-1034 抑制高度表达 p-MET 的肿瘤增殖。NPS-1034 处理可明显减少肿瘤的血管形成。在用 NPS-1034 处理的小鼠的肿瘤切片中,α-平滑肌肌动蛋白 (α-SMA) 的表达降低。NPS-1034 处理的小鼠几乎没有体重减轻,这表明 NPS-1034 通常具有良好的耐受性[2]

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

分子量

551.54

Formula

C31H23F2N5O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 34 mg/mL (61.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

To perform the MTT assay, cells (0.5×104/well) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader[1].

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

Animal Administration
[1]

Female severe combined immunodeficiency (SCID) mice (17 to 20 g, 6 weeks of age) are used. Tumors are grown by implanting 5×106 cells in Matrigel into the mouse flanks. Treatment of 5 mice per group is started when the tumors have reached a volume of 50 to 100 mm3 with vehicle control or NPS-1034 (10 mg/kg, 5 days a week). NPS-1034 is administered orally. Treatment is stopped at the indicated day and mice are followed-up for tumor recurrence. To measure tumor size, the length (L) and width (W) of the tumor are measured with calipers, and tumor volume (TV) is calculated as TV=(L×W2)/2. Immunohistochemical staining is performed using a specific primary antibody, the EnVision Plus staining kit, and the APO-Direct terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling assay kit, according to the suppliers' instructions. Quantitative analysis of section staining is performed by counting immunopositive cells in 5 arbitrarily selected fields at ×40 magnification[1].

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8131 mL 9.0655 mL 18.1311 mL 45.3276 mL
5 mM 0.3626 mL 1.8131 mL 3.6262 mL 9.0655 mL
10 mM 0.1813 mL 0.9066 mL 1.8131 mL 4.5328 mL
15 mM 0.1209 mL 0.6044 mL 1.2087 mL 3.0218 mL
20 mM 0.0907 mL 0.4533 mL 0.9066 mL 2.2664 mL
25 mM 0.0725 mL 0.3626 mL 0.7252 mL 1.8131 mL
30 mM 0.0604 mL 0.3022 mL 0.6044 mL 1.5109 mL
40 mM 0.0453 mL 0.2266 mL 0.4533 mL 1.1332 mL
50 mM 0.0363 mL 0.1813 mL 0.3626 mL 0.9066 mL
60 mM 0.0302 mL 0.1511 mL 0.3022 mL 0.7555 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NPS-1034
目录号:
HY-100509
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