產(chǎn)品描述: | SB-743921 hydrochloride is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. |
靶點(diǎn): |
Eg5:0.1 nM (Ki);Kinesin;?KSP |
體內(nèi)研究: |
SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts |
參考文獻(xiàn): |
1. Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006. 2. Yin Y, et al. Kinesin spindle protein inhibitor SB743921 induces mitotic arrest and apoptosis and overcomes imatinib resistance of chronic myeloid leukemia cells. Leuk Lymphoma. 2015 Jun;56(6):1813-20. 3. Good JA, et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem. 2013 Mar 14;56(5):1878-93. |
溶解性: |
DMSO : ≥ 100 mg/mL (180.66 mM) H2O : 10 mg/mL (18.07 mM; ultrasonic and warming and heat to 60°C) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.807 ml |
9.033 ml |
18.066 ml |
5 mM |
0.361 ml |
1.807 ml |
3.613 ml |
10 mM |
0.181 ml |
0.903 ml |
1.807 ml |
50 mM |
0.036 ml |
0.181 ml |
0.361 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。 |