| 產(chǎn)品描述： | Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'. |
| 靶點(diǎn)： |
CK2α:1 nM (IC50);CK2α':1 nM (IC50);CaseinKinase;Autophagy |
| 體內(nèi)研究： |
Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models |
| 參考文獻(xiàn)： |
1. Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98. 2. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40. 3. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70. |
| 溶解性： |
DMSO : ≥ 35 mg/mL (100.07 mM) 0.1 M NaOH : 33.33 mg/mL (95.29 mM; ultrasonic and adjust pH to 9 with NaOH) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.859 ml |
14.295 ml |
28.59 ml |
| 5 mM |
0.572 ml |
2.859 ml |
5.718 ml |
| 10 mM |
0.286 ml |
1.43 ml |
2.859 ml |
| 50 mM |
0.057 ml |
0.286 ml |
0.572 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。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京