| 貨號 | 規(guī)格 | 價格 | 上海 | 北京 | 武漢 | 南京 | 購買數(shù)量 |
|---|---|---|---|---|---|---|---|
S81037-1mg |
99.9% | ￥240.00 | 10 | - | - | - |
|
S81037-2mg |
99.9% | ￥400.00 | 10 | - | - | - |
|
S81037-5mg |
99.9% | ￥640.00 | 8 | - | - | - |
|
S81037-10mg |
99.9% | ￥960.00 | 7 | - | - | - |
|
S81037-25mg |
99.9% | ￥1680.00 | 7 | - | - | - |
|
S81037-50mg |
99.9% | ￥2880.00 | 5 | - | - | - |
|
S81037-100mg |
99.9% | ￥4800.00 | 4 | - | - | - |
|
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line
| 產(chǎn)品描述： | Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點： | ERK2:0.3 nM (IC50, at KM ATP (60 μM));ERK1;ERK | ||||||||||||||||||||
| 體外研究： | Combined Ulixertinib (BVD-523; 10, 20, 30 μM; 48 hours) and VS-5584 treatment causes significant induction of cell death in human pancreatic cancer (HPAC) cells in PDAC cell lines BxPC-3, MIAPaCa-2, and CFPAC-1 | ||||||||||||||||||||
| 體內(nèi)研究： | In the pharmacokinetic study, the sensitivity and specificity of the assay are found to be sufficient for accurately characterizing the plasma pharmacokinetics of Ulixertinib (VRT752271) in Balb/C mice | ||||||||||||||||||||
| 參考文獻： | 1. Ward RA, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58(11):4790-801. 2. Kumar R, et al. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2016 Jun 5;125:140-4. 3. Changwen Ning, et al. Targeting ERK Enhances the Cytotoxic Effect of the Novel PI3K and mTOR Dual Inhibitor VS-5584 in Preclinical Models of Pancreatic Cancer. Oncotarget. 2017 Jul 4;8(27):44295-44311. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存條件： | -20℃ | ||||||||||||||||||||
| 配置溶液濃度參考： |
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| 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
滬公網(wǎng)安備 31011702002021號
危險品化學品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京