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ERK-IN-3 benzenesulfonate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ERK-IN-3 benzenesulfonate图片
CAS NO:2055597-39-0
包装与价格:
包装价格(元)
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ERK-IN-3 benzenesulfonate 是一种有效和具有口服活性的 ERK 抑制剂。 ERK-IN-3 benzenesulfonate 以较低的 IC50 值抑制 ERK1/2。 ERK-IN-3 benzenesulfonate 可用于研究由 RAS 突变驱动的癌症。
Cas No.2055597-39-0
分子式C28H31ClFN7O5S
分子量632.11
溶解度DMSO : 320 mg/mL (506.24 mM; Need ultrasonic)
储存条件-20°C, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1].

ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1].ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1].

ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].

[1]. Sanjeeva PR, et, al. Abstract B150: ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. Molecular Cancer Therapeutics. 2018 Jan; 17(1).

 
 
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