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NPS-1034 纯度: ≥98.0%
NPS-1034 是 AXL 和 MET 的双重抑制剂,其 IC50 值分别为 10.3 和 48 nM。
NPS-1034 Chemical Structure
CAS No. : 1221713-92-3
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10 mM * 1 mL in DMSO | ¥1201 | In-stock | |
5 mg | ¥990 | In-stock | |
10 mg | ¥1550 | In-stock | |
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NPS-1034 相关产品
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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] |
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体外研究 (In Vitro) |
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[1]. 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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
551.54 |
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Formula |
C31H23F2N5O3 |
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CAS 号 |
1221713-92-3 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 34 mg/mL (61.65 mM; Need ultrasonic) 配制储备液
*
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。 |
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参考文献 |
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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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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