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CCT196969 是泛-Raf 抑制剂,抑制B-Raf、BRafV600E 和CRAF,IC50分别为 0.1、0.04、和 0.01 μM。
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CCT196969 是泛-Raf 抑制剂,抑制B-Raf、BRafV600E 和CRAF,IC50分别为 0.1、0.04、和 0.01 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 218 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 787 | 现货 | |
25 mg | ¥ 1,490 | 现货 | |
50 mg | ¥ 2,280 | 现货 | |
100 mg | ¥ 3,270 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 562 | 现货 |
产品描述 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
靶点活性 | B-Raf (V600E):0.04 μM, Lck:0.02 μM, Raf:0.01 μM, BRAF:0.1 μM, Src:0.03 μM |
体外活性 | CCT196969促进caspase 3及PARP的切割,从而诱导细胞凋亡。CCT196969不激活悖论途径,且在BRAF和NRAS突变的黑色素瘤中抑制MEK/ERK通路。对于BRAF突变的黑色素瘤和结直肠癌细胞株,CCT196969显示出活性,但对于BRAF和NRAS野生型的癌细胞则无效。 |
体内活性 | 口服CCT196969,每日10 mg/kg,24小时后可在血浆中测得约1 μM浓度。其口服生物利用度约为55%。在评估的剂量下,CCT196969极为安全耐受,且在体内不产生任何显著不良效应。 |
细胞实验 | Cell lines: cell line derived from a vemurafenib-resistant melanoma. Method: The three cell lines derived from tumors displaying resistance to vemurafenib are incubated with DMSO (control),PLX4720,CCT196969,or CCT241161 (1 μM; 4 hr).Protein extracts are prepared in CLB1 lysis buffer,and samples are analyzed by Zeptosens RPPA(reverse phase protein arrays). |
动物实验 | Animal Models: CD-1 mice. Formulation: 5% DMSO,95% water. Dosages: 20 mg/kg . Administration: oral gavage |
分子量 | 513.52 |
分子式 | C27H24FN7O3 |
CAS No. | 1163719-56-9 |
Smiles | CC(C)(C)c1cc(NC(=O)Nc2ccc(Oc3ccnc4[nH]c(=O)cnc34)cc2F)n(n1)-c1ccccc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: Insoluble DMSO: 100 mg/mL (194.73 mM) H2O: Insoluble | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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