化合物 RKI-1447 dihydrochloride,RKI-1447 dihydrochloride

化合物 RKI-1447 dihydrochloride|T61905|TargetMol

價(jià)格	￥595	￥295
包裝	5mg	2mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱(chēng):化合物 RKI-1447 dihydrochloride	英文名稱(chēng):RKI-1447 dihydrochloride
CAS:1782109-09-4	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Shipping with blue ice.
產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T61905

Product Introduction

Bioactivity

Name	RKI-1447 dihydrochloride
Description	RKI 1447 dihydrochloride is an effective and selective ROCK inhibitor (ROCK1 IC50=14.5 nM, ROCK2 IC50=6.2 nM). RKI 1447 dihydrochloride can inhibit the growth of colorectal cancer cells and promote cell apoptosis.
In vitro	RKI 1447 suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μM [1]. RKI 1447 (0.003-10 μM) is potent at inhibiting the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells [1]. RKI 1447 exhibits effective anticancer activity in colorectal carcinoma (CRC). RKI 1447 (10-320 μM; 24 hours) drastically suppresses HCT-8 and HCT-116 cell growth [2]. RKI 1447 (20-80 μM; 24 hours) induces apoptosis in a dose-dependent manner [2]. Cell Viability Assay [2] Cell Line: CRC cell lines HCT-8 and HCT-116 cells Concentration: 0, 10, 20, 40, 80, 160, 320 μM Incubation Time: 24 hours Result: HCT-8 and HCT-116 viability was drastically decreased in a dose-dependent manner. Apoptosis Analysis [2] Cell Line: CRC cell lines HCT-8 and HCT-116 cells Concentration: 0, 20, 40, 80 μM Incubation Time: 24 hours Result: Treatment promoted apoptosis. Western Blot Analysis [1] Cell Line: MDA-MB-231 human breast cancer cells Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3,10 μM Incubation Time: Result: Decreased the levels of P-MLC-2, but not total MLC-2, in a concentration-dependent manner with significant effects starting at 100 nM.
In vivo	RKI 1447 (200 mg/kg; i.p. daily for 14 days) inhibits mammary tumor growth in vivo [1]. RKI 1447 (100 mg/kg; i.p.; once every 3 days; for 14 days) exerts antitumor activity on CRC in vivo. RKI 1447 does not exert physiological toxicity on the mice [2]. Animal Model: MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J] [1] Dosage: 200 mg/kg Administration: Treated i.p. daily for 14 days Result: Tumors from mice treated with vehicle increased in size with an average percent change in tumor volume of 68.3%. In contrast, tumors from mice treated with the RKI-1447 increased in size with an average percent change in tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87%. Animal Model: 5-week-old Male BALB/C nude mice [2] Dosage: 100 mg/kg Administration: Intraperitoneally injected; once every 3 days; for 14 days Result: Efficiently blocked CRC tumor growth in vivo.
Storage	Shipping with blue ice.

關(guān)鍵字： RKI-1447 dihydrochloride|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶(hù)群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶(hù)的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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