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BMS-345541
CAS No. 547757-23-3
BMS-345541 ( BMS345541 hydrochloride | BMS-345541 hydrochloride | BMS 345541 hydrochloride )
产品货号. M14971 CAS No. 547757-23-3
一种有效的选择性 IKK-2 抑制剂，IC50 为 0.3 uM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥389 | 有现货 |
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| 5MG | ￥640 | 有现货 |
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| 10MG | ￥1037 | 有现货 |
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| 25MG | ￥1912 | 有现货 |
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| 50MG | ￥3208 | 有现货 |
|
| 100MG | ￥4803 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称BMS-345541
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述一种有效的选择性 IKK-2 抑制剂，IC50 为 0.3 uM。
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产品描述A potent and selective IKK-2 inhibitor with IC50 of 0.3 uM; less potent for IKK-1 (IC40=4 uM) and no activity against IKK-ε; inhibits LPS-stimulated TNFα, IL-1β, IL-8, and IL-6 in THP-1 cells with IC50 of1-5 uM; has excellent pharmacokinetics in mice.
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体外实验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. 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.
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体内实验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. 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. BMS-345541 (30 and 100 mg/kg, p.o.) is effective in blocking both clinical and histological endpoints of inflammation and injury in mice.
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同义词BMS345541 hydrochloride | BMS-345541 hydrochloride | BMS 345541 hydrochloride
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通路Immunology/Inflammation
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靶点IκB kinase (IKK)
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受体IκB kinase (IKK)
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研究领域Cancer
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适应症——
化学信息
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CAS Number547757-23-3
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分子量291.7792
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分子式C14H18ClN5
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN.Cl
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化学全称1,2-Ethanediamine, N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-, hydrochloride (1:1)
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Burke JR, et al. J Biol Chem. 2003 Jan 17;278(3):1450-6.
2. McIntyre KW, et al. Arthritis Rheum. 2003 Sep;48(9):2652-9.
3. López-Guerra M, et al. Clin Cancer Res. 2009 Apr 15;15(8):2767-76.
产品手册
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