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别名 | RG7420,XL518 | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C21H21F3IN3O2 |
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分子量 | 531.31 | CAS号 | 934660-93-2 | ||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (188.21 mM) | ||||
Ethanol | 17 mg/mL (31.99 mM) | ||||||
Water | Insoluble | ||||||
体内(现配现用) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | Cobimetinib (GDC-0973, RG7420)是一种有效的高选择性MEK1抑制剂,IC50 为 4.2 nM,且对其他很多丝氨酸-苏氨酸和酪氨酸激酶没有显著抑制作用。Cobimetinib 可诱导凋亡。Phase 3。 | ||
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靶点 |
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体外研究 | Cobimetinib对一组广泛类型的肿瘤细胞的生长表现出强烈的抑制活性,特别是对BRAF或KRAS突变型癌细胞系。结合GDC-0941,GDC-0973在888MEL和A2058细胞中导致生存能力降低,通路抑制,以及细胞凋亡增加。[1] GDC-0973和vemurafenib联合给药显著增加所有BRAFV600E系中细胞膜上减少的GLUT-1水平。[2] |
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体内研究 | 在负荷BRAFV600E和KRAS突变型肿瘤的小鼠体内,Cobimetinib (10 mg/kg, p.o.)产生抗肿瘤作用,结合GDC-0973和GDC-0941能够提高疗效。[1] 在负荷耐药的A375异种移植物小鼠体内,GDC-0973与GDC-0941结合诱导己糖激酶II,c-RAF,Ksr 和p-MEK蛋白质的水平减少。[2] |
动物实验 | 动物模型 | 负荷Molm-13,Molm-16,MX-1,DLD-1,HCT-116,LoVo,FaDu,537MEL,A2058,A2058-X1,A375,A375.X1,A427,A549,Calu-6,EBC-1,NCI-H441,NCI-H2122,NCI-H460,NCI-H520.X1,SKOV-3,KP4-X1.1,MiaPaCa-2,22Rv1,DU-145.X1,S,NCI-H69 异种移植瘤的小鼠 |
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剂量 | 10 mg/kg | |
给药处理 | p.o. |
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数据来源于[Data independently produced by , , Mol Cell Proteomics, 2017, 16(2):265-277]
数据来源于[Data independently produced by , , Cell Physiol Biochem, 2018, 47(2):680-693]
数据来源于[Data independently produced by , , PLoS One, 2017, 12(11):e0186981]
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Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, S2666-3791(23)00367-1] | PubMed: 37734378 |
An in vivo avian model of human melanoma to perform rapid and robust preclinical studies [ EMBO Mol Med, 2023, 15(3):e16629] | PubMed: 36692026 |
Irreversible HER2 inhibitors overcome resistance to the RSL3 ferroptosis inducer in non-HER2 amplified luminal breast cancer [ Cell Death Dis, 2023, 14(8):532] | PubMed: 37596261 |
The antiviral effects of a MEK1/2 inhibitor promote tumor regression in a preclinical model of human papillomavirus infection-induced tumorigenesis [ Antiviral Res, 2023, 216:105667] | PubMed: 37429527 |
Understanding cancer drug resistance with Sleeping Beauty functional genomic screens: Application to MAPK inhibition in cutaneous melanoma [ iScience, 2023, 26(10):107805] | PubMed: 37860756 |
High-Throughput Functional Evaluation of MAP2K1 Variants in Cancer [ Mol Cancer Ther, 2023, 22(2):227-239] | PubMed: 36442478 |
USP10 Regulates ZEB1 Ubiquitination and Protein Stability to Inhibit ZEB1-Mediated Colorectal Cancer Metastasis [ Mol Cancer Res, 2023, 21(6):578-590] | PubMed: 36940483 |
Identifying Potential Molecular Targets in Fungi Based on (Dis)Similarities in Binding Site Architecture with Proteins of the Human Pharmacolome [ Molecules, 2023, 28(2)692] | PubMed: 36677748 |
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