CAS NO: | 547757-23-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits ofIKK(IKK-2IC50=0.3 μM,IKK-1IC50=4 μM). BMS-345541 binds at an allosteric site ofIKK. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | BMS-345541 inhibits IKK-2 and IKK-1 in dose-dependent manner. BMS-345541 fails to inhibit a panel of both serine/threonine and tyrosine kinases at concentrations as high as 100 μM. MS-345541 at concentrations as high as 100 μM fails to block both the anisomycin-stimulated phosphorylation of c-Jun and LPS-stimulated activation of MAPKAP K2 in THP-1 cells, as well as the EGF-stimulated phosphorylation of STAT3 in H292 cells[1]. BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells. BMS-345541 (0, 100 μM) shows apoptotic features as revealed by TUNEL staining and nuclear condensation[2]. | ||||||||||||||||
体内研究 (In Vivo) | BMS-345541 (10 mg/kg, p.o.) results in prolonged serum drug levels, with concentrations sustained at or above 1 μM for many hours in mice. BMS-345541 dose-dependently inhibits the production of TNFα measured in the serum of animals challenged with an intraperitoneal administration of LPS[1]. BMS-345541 (0, 10, 25, and 75 mg/kg, p.o.) effectively inhibits SK-MEL-5 tumor growth in a dose-dependent manner in the mice. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 show effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86±2.8%, 69±11% and 67±3.4%, respectively[2]. BMS-345541 (30 and 100 mg/kg, p.o.) is effective in blocking both clinical and histological endpoints of inflammation and injury in mice[3]. | ||||||||||||||||
分子量 | 291.78 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C14H18ClN5 | ||||||||||||||||
CAS 号 | 547757-23-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 50 mg/mL(171.36 mM;Need ultrasonic) DMSO : 20 mg/mL(68.54 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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