產(chǎn)品目錄

規(guī)格	5mg 25mg
CAS	181223-80-3
別名
化學(xué)名	N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide
分子式	C26H28N4O3
分子量	444.53
溶解度	DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: slightly soluble
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

DEL-22379 is an inhibitor of the dimerization of ERK with IC50 values ranging from 150-400 nM regardless of genotypes in oncogenic cells [1].

As an spatial regulator of ERK signals, ERK dimerization is essential. Impeding ERK dimerization can result in the impeding of ERK signals’ extranuclear component and hence result in curtailing tumor development and cellular transformation [1].

In HEK293 cells, DEL-22379 abolished EGF-stimulated ERK dimerization. In these cells, the EGF-induced co-immunoprecipitation of hemagglutinin- or FLAG epitopes- tagged ectopic ERK2 molecules, was abolished by DEL-22379 with an IC50 value of ~0.5 µM. In both assays, the inhibition of DEL-22379 to ERK dimerization was not associated with ERK phosphorylation. In the cytoplasm of EGF-stimulated HeLa cells, ERK dimerization was prominent, but previous treatment with DEL-22379 also resulted in no detected ERK dimmers [1].

In nude mice with some of the aforementioned tumor cell lines, DEL-22379 at a dose of 15 mg/kg inhibited ERK dimerization evidently in xenografted tumors and in liver extracts. DEL-22379 inhibited the tumor progression of A375 cells (BRAF mutant) markedly. Activated-RAS-driven tumors were very sensitive to DEL-22379. Data indicated that tumorigenesis had greater requirements for ERK dimerization than for proliferation. In tumors, treatment with DEL-22379 resulted in extensive mucinous differentiation and cell death [1].

Reference:

[1]. Herrero A, Pinto A, Colón-Bolea P, et al. Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes. Cancer cell, 2015, 28(2): 170-182.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國(guó)有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請(qǐng)您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對(duì)產(chǎn)品有任何疑問(wèn),也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請(qǐng)輸入您對(duì)我們的意見(jiàn)或建議*
驗(yàn)證碼*