Glumetinib
Glumetinib(Glumetinib)
CAS: 1642581-63-2
化学式: C21H17N9O2S
| 中文名 | Glumetinib |
| 英文名 | Glumetinib |
| 别名 | 谷美替尼 化合物GLUMETINIB 6-(1-甲基-1H-吡唑-4-基)-1-((6-(1-甲基-1H-吡唑-4-基)咪唑并[1,2-A]吡啶-3-基)磺酰基)-1H-吡唑[4,3-B]吡啶 |
| 英文别名 | SCC244 Glumetinib Gumarontinib GLUMETINIB (SCC244) 6-(1-Methyl-1H-pyrazol-4-yl)-1-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)sulfonyl)-1H-pyrazolo[4,3-b]pyridine 1H-Pyrazolo[4,3-b]pyridine, 6-(1-methyl-1H-pyrazol-4-yl)-1-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl]- |
| CAS | 1642581-63-2 |
| 化学式 | C21H17N9O2S |
| 分子量 | 459.48 |
| 密度 | 1.61±0.1 g/cm3(Predicted) |
| 溶解度 | 溶于DMSO (>25 mg/ml) |
| 酸度系数 | 0.09±0.10(Predicted) |
| 存储条件 | -20°C |
| 稳定性 | 稳定1年的供应。DMSO中的溶液可以在-20 °C下储存长达1个月。 |
| 外观 | 固体 |
| 颜色 | Beige |
| 靶点 | IC50: 0.42 nM (c-Met kinase) |
| 体外研究 | 在具有扩增MET基因的EBC-1、MKN-45细胞和HGF刺激的U87MG细胞中，SCC244强烈抑制c-Met、AKT和ERK磷酸化。SCC244可对c-Met驱动的癌细胞增殖有选择性和深刻影响。SCC244抑制依赖于c-Met的诸如转移和血管生成等肿瘤表型。 |
| 体内研究 | 在人源肿瘤细胞或非小细胞肺癌的移植瘤模型中、或是由MET异常所驱动的肝癌患者肿瘤组织中，SCC244在各种耐受剂量下都具有强效的抗肿瘤活性。SCC244可通过抗增殖和抗血管新生抑制c-MET下游通路。 |
| 参考资料 展开查看 | [1]. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762. |
Glumetinib - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.176 ml | 10.882 ml | 21.764 ml |
| 5 mM | 0.435 ml | 2.176 ml | 4.353 ml |
| 10 mM | 0.218 ml | 1.088 ml | 2.176 ml |
| 5 mM | 0.044 ml | 0.218 ml | 0.435 ml |
最后更新：2024-01-02 23:10:35
Glumetinib - 细胞实验
Cells were seeded in 96-well plates at a low density in growth media. The next day, appropriate controls or designated concentrations of compounds were added to each well, and the cells were incubated for 72 hours. HUVECs (passage 3) were seeded in 96-well plates in growth media overnight and transferred to serum-free media for 24 hours. The following day, appropriate controls or designated concentrations of compounds were added to each well, and HGF was added to designated wells at 100 ng/mL. The cells were incubated for 48 hours. Finally, cell proliferation was determined using a sulforhodamine B assay, a thiazolyl blue tetrazolium bromide assay or a cell counting kit (CCK-8) assay.
最后更新：2023-08-16 21:32:38
Glumetinib - 动物实验
To assess the pharmacodynamics of SCC244 in tumors, mice bearing established xenograft tumors were treated with a single dose of the compound at 10 or 2.5 mg/kg, and tumors were harvested at several time points. At a designated time following administration, mice were humanely euthanized, and their tumors were resected. The tumors were snap-frozen in liquid nitrogen and then homogenized in 500 μL of protein extraction solution (radioimmunoprecipitation assay, RIPA). The tumor extracts were then subjected to Western blot analysis. The individual bands of phospho-c-Met, phospho-AKT, and phospho-ERK were scanned and quantified using Gel Pro Analyzer software. The relative tyrosine phosphorylation of each sample at the indicated time points was then calculated, with the average value of vehicle-treated sample used as 100%.
最后更新：2023-08-16 21:32:38
供应商列表
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 北京
包装: 盒
规格: IG1620-1mg,1mg
价格: 电话、微信、QQ、邮件
库存: 现询
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 索莱宝直销，欢迎来询
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 上海
规格: G795743
价格: 1ml-786,10mg-425,50mg-1079
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 上海
规格: 98%
价格: 5mg 480,10mg 800,25mg 1600,100mg 4800
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: Glumetinib 98% MedMol 货号：S88460
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 北京
包装: 盒
规格: IG1620-1mg,1mg
价格: 电话、微信、QQ、邮件
库存: 现询
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 索莱宝直销，欢迎来询
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 上海
规格: G795743
价格: 1ml-786,10mg-425,50mg-1079
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
QQ: 2885703204/288570320
微信: 19863730987/17821173903
现货供应
产品名: Glumetinib 去供应商网站查看 询盘CAS: 1642581-63-2
产地: 上海
规格: 98%
价格: 5mg 480,10mg 800,25mg 1600,100mg 4800
库存: 现货
电话: 18301782025
手机: 18301782025
电子邮件: 3008007403@qq.com
QQ: 3008007403
微信: 18301782025
产品描述: Glumetinib 98% MedMol 货号：S88460
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