S80981 |
GNF-7 |
源葉(MedMol) | 97% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies
- 靶點(diǎn): IC50: 133 nM (Bcr-AblWT); 61 nM (Bcr-AblT315I); 25 nM (ACK1); 8 nM (GCK);Bcr-Abl;ACK;AChR
- 體內(nèi)研究:
GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg). GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)
- 參考文獻(xiàn):
1. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. 2. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I gatekeeper mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48. 3. Cho, H., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.826 ml 9.132 ml 18.264 ml 5 mM 0.365 ml 1.826 ml 3.653 ml 10 mM 0.183 ml 0.913 ml 1.826 ml 50 mM 0.037 ml 0.183 ml 0.365 ml
- 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。
輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)