Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 9,500 | |||
5 mg | 在庫あり | ¥ 15,500 | |||
10 mg | 在庫あり | ¥ 23,000 | |||
25 mg | 在庫あり | ¥ 45,500 | |||
50 mg | 在庫あり | ¥ 80,000 | |||
100 mg | 在庫あり | ¥ 119,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 16,000 |
説明 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
ターゲット&IC50 | BRAF:0.1 μM, Raf:0.01 μM, Lck:0.02 μM, Src:0.03 μM, B-Raf (V600E):0.04 μM |
In vitro | CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS. |
In vivo | Oral dosing at 10 mg/kg/day of CCT196969 results in plasma concentrations ~1 μM at 24 hr. It is orally bioavailable at ~55%. CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo. |
細胞研究 | 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). |
動物実験 | 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: Insoluble
DMSO: 100 mg/mL (194.73 mM)
H2O: Insoluble
You can also refer to dose conversion for different animals. 詳細
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CCT196969 1163719-56-9 Angiogenesis MAPK Tyrosine Kinase/Adaptors Raf Src CCT 196969 Inhibitor inhibit CCT-196969 Raf kinases inhibitor