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Capmatinib (INCB28060) 卡马替尼;苯扎米特

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Capmatinib (INCB28060) 是一种新型, ATP竞争性的c-MET抑制剂,IC50为0.13 nM,Capmatinib 可抑制 c-MET 的磷酸化,以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。

Capmatinib (INCB28060)结构式

别名:INC280; Capmatinib; NVP-INC280

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
2mg ¥ 364 中国库存现货
5mg ¥ 637 中国库存现货
10mg ¥ 884 中国库存现货
25mg ¥ 1274 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Capmatinib (INCB28060)是一种新型, ATP竞争性的c-MET抑制剂,IC50为0.13 nM,Capmatinib 可抑制 c-MET 的磷酸化,以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib (INCB28060) 具有皮摩尔酶活效价,对 c-MET选择性比其它大部分人源激酶高出10000多倍。在肿瘤细胞里 INCB28060 可以抑制c-MET磷酸化以及c-MET介导的信号转导。Capmatinib (INCB28060) 抑制 c-MET依赖的细胞增殖和存活并且抑制anchorage非依赖性肿瘤细胞生长和细胞迁移。

使用AbMole产品发表的文献
产品使用成果展示
数据来源 Mol Cancer Ther (2017). Figure 4. INCB28060 (Abmole Bioscience. Houston, TX, USA)
方法 oral gavage
细胞系/动物模型 KPC and orthotopic transplant model mice
浓度 1 mg/kg
处理时间 7, 14 or 21 days
实验结果 Importantly, the group with dual inhibitor treatment in addition to gemcitabine showed no metastases. This result suggests that the combination of c-Met and Hh inhibitors in addition to gemcitabine has significantly suppressed metastasis formation.
数据来源 Mol Cancer Ther (2017). Figure 3. INCB28060 (Abmole Bioscience. Houston, TX, USA)
方法 oral gavage
细胞系/动物模型 KPC and orthotopic transplant model mice
浓度 1 mg/kg
处理时间 7, 14 or 21 days
实验结果 These results suggest that the resistance to the c-Met and Hh inhibitor is developed following a prolonged treatment of each individual inhibitor; however, the resistance may be overcome by combining both c-Met and Hh inhibitors.
数据来源 Mol Cancer Ther (2017). Figure 1. INCB28060 (Abmole Bioscience. Houston, TX, USA)
方法 oral gavage
细胞系/动物模型 KPC and orthotopic transplant model mice
浓度 1 mg/kg
处理时间 7, 14 or 21 days
实验结果 The data suggest that combination of both inhibitors with gemcitabine shows a trend in shrinkage of primary tumor volume in both mouse models of PDA after one week of treatment regimen.
数据来源 Can Res (2017). Figure 3.INC280 (Abmole Bioscience).
方法
细胞系/动物模型 PDAC cells
浓度
处理时间
实验结果 As expected, neither the Hh inhibitor nor the HGF/c-Met inhibitor affected the levels of total AnxA2 or P-Y23-AnxA2 in Panc10.05 cells in the singly cultured serum-reduced media (Fig. 3A and B; Supplementary Fig. S5E and S5F). It is likely the concentration of HGFand IGF-1 in serum-reduced media is lower than the effective thresholds.
数据来源 Nature (2015). Figure 3. PF-04217903 and INCB28060 (AbMole Bioscience)
方法 mice treatment in vivo and histological evaluation
细胞系/动物模型 B16F10 cells
浓度 40mg/kg PF-04217903 and 50mg/kg INCB28060
处理时间 2 weeks
实验结果 Systemic treatment of WT mice carrying B16F10 melanomas (which are dependent on MET14) with three different MET tyrosine-kinase inhibitors (PF-04217903, INCB28060 and JNJ-38877605), strongly reduced TAN recruitment .
数据来源 Nature (2015). Figure 2. PF-04217903 and INCB28060 (AbMole Bioscience)
方法 mice treatment in vivo and histological evaluation
细胞系/动物模型 B16F10 cells
浓度 40mg/kg PF-04217903
处理时间 2 weeks
实验结果 "Systemic administration of PF-04217903 decreased the weight and volume of B16F10 melanomas by 36% and 54%, respectively. Instead, MET knockdown in cancer cells only, led to 58% and 75% inhibition of tumour growth and volume.TAN inhibition by PF-04217903 was comparable in both Met-silenced and scrambled B16F10 melanomas."
实验参考
体外实验*
细胞系 SUN-5 and SUN-1 cells
方法 Optimal cell density used in the viability assay was predetermined for individual cell lines. To determine compound potency, cells were seeded into 96-well microplates at the appropriate density in media containing 1% to 2% FBS and supplemented with serial dilutions of INCB28060 in a final volume of 100 μL per well. After 72-hour incubation, 24 μL of CellTiter 96 AQueous One Solution (Promega) was added to each well, and the plates were incubated for 2 hours in a 37°C incubator. The optical density was measured in the linear range using a microplate reader at 490 nm with wavelength correction at 650 nm. IC50 values were calculated using the GraphPad Prism Software.
浓度 0~333 nM
处理时间 3 days

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 B16F10 tumour-bearing mice
配制 0.5% methylcellulose in saline
剂量 50mg/kg INCB28060
给药处理 via oral gavage every day once a day starting from day 2 after tumour injection and twice a day from day 11 until the end of the experiment(2 weeks)

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 412.42
分子式 C23H17FN6O
CAS号 1029712-80-8
溶解性(25°C) DMSO 15 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4247 mL 12.1236 mL 24.2471 mL
5 mM 0.4849 mL 2.4247 mL 4.8494 mL
10 mM 0.2425 mL 1.2124 mL 2.4247 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Sung-Hwa Sohn, et al. BMC Res Notes. INC280 inhibits Wnt/β-catenin and EMT signaling pathways and its induce apoptosis in diffuse gastric cancer positive for c-MET amplification

[2] Sabrina Baltschukat, et al. Clin Cancer Res. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation

[3] Liu X, et al. Clin Cancer Res. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.

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关键词:Capmatinib (INCB28060), INC280; Capmatinib; NVP-INC280, Capmatinib (INCB28060)供应商, c-Met抑制剂, 购买Capmatinib (INCB28060), Capmatinib (INCB28060)溶解度, Capmatinib (INCB28060)结构式








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