貨號	規格	價格	上海	北京	武漢	南京
S81037-1mg	99.9%	￥240.00 S81037-1mg ￥240.00 現貨	10 10	-	-	-
S81037-2mg	99.9%	￥400.00 S81037-2mg ￥400.00 現貨	10 10	-	-	-
S81037-5mg	99.9%	￥640.00 S81037-5mg ￥640.00 現貨	8 8	-	-	-
S81037-10mg	99.9%	￥960.00 S81037-10mg ￥960.00 現貨	7 7	-	-	-
S81037-25mg	99.9%	￥1680.00 S81037-25mg ￥1680.00 現貨	7 7	-	-	-
S81037-50mg	99.9%	￥2880.00 S81037-50mg ￥2880.00 現貨	5 5	-	-	-
S81037-100mg	99.9%	￥4800.00 S81037-100mg ￥4800.00 現貨	4 4	-	-	-

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產品介紹

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

產品描述：

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：

	1mg	5mg	10mg
1 mM	2.308 ml	11.539 ml	23.077 ml
5 mM	0.462 ml	2.308 ml	4.615 ml
10 mM	0.231 ml	1.154 ml	2.308 ml
50 mM	0.046 ml	0.231 ml	0.462 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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