化合物 CI-1040|T2443|TargetMol

價(jià)格	￥198	￥443	￥745
包裝	1mg	5mg	10mg

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:化合物 CI-1040	英文名稱:CI-1040
CAS:212631-79-3	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.1%	產(chǎn)品類別: 抑制劑
貨號(hào): T2443

Product Introduction

Bioactivity

名稱	CI-1040
描述	CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).
細(xì)胞實(shí)驗(yàn)	Cells were planted seeded in T-75 cm2 flasks and treated the next day for 24 h with either DMSO or PD 184352. Single-cell suspensions were collected, and pellets were fixed in ice-cold ethanol (70%) for 30 min. After centrifugation of the samples, propidium iodide (50 μg/ml) and RNase (30 units/ml) were added to the pellets for 20 min at 37 °C. After filtration, samples were analyzed by flow cytometry [1].
激酶實(shí)驗(yàn)	All protein kinase activities were linear with respect to time in every incubation. Assays were performed either manually for 10 min at 30 °C in 50 μl incubations using [γ-32P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 min at ambient temperature in 25 μl incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate were 0.1 mM and 10 mM respectively, unless stated otherwise. This concentration of ATP is 5–10-fold higher than the Km for ATP of most of the protein kinases studied in the present paper, but lower than the normal intracellular concentration, which is in the millimolar range. All assays were initiated with MgATP. Manual assays were terminated by spotting aliquots of each incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays were terminated by the addition of 5 μl of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers were then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity [2].
動(dòng)物實(shí)驗(yàn)	Tumor fragments (approximately 3 mm^3 in size) were implanted subcutaneously into the right axillae of CD2F1 male mice (colon 26 studies) or female nude mice (HT-29 studies) 4–6 weeks old. Treatment was administered by gavage or intraperitoneally and was initiated either the day after tumor implantation (colon 26) or when tumors reached approximately 200 mg in size (HT-29). PD 184352 was prepared in a vehicle of 10% Cremophore EL, 10% ethanol and 80% water. Tumor size was evaluated periodically by caliper measurements, generally three times per week. Percent tumor growth inhibition was calculated as [(T–C)/number of days of treatment] × 100, with T and C being defined as the time required for treated and control tumors, respectively, to reach 750 mg (colon 26) or to reach twofold growth (HT-29) [1].
體外活性	PD 184352（CI-1040）顯著降低了在血清存在條件下生長(zhǎng)的多種腫瘤細(xì)胞系中磷酸化MAPK（pMAPK）的穩(wěn)態(tài)水平。在含1 μM PD 184352 的培養(yǎng)基中處理結(jié)腸26細(xì)胞1小時(shí)，可使pMAPK水平降低超過(guò)75%。用10 μM PD 184352處理結(jié)腸26細(xì)胞，不會(huì)抑制Jun激酶、p38激酶或AKT的磷酸化[1]。PD 184352抑制MKK1的IC50為0.3 μM，這比抑制Swiss 3T3細(xì)胞中EGF誘導(dǎo)的ERK2活化所需濃度高出15倍。在2 nM PD 184352 的作用下，MKK1在細(xì)胞中的活化被50%抑制[2]。CI-1040以劑量和時(shí)間依賴的方式誘導(dǎo)U-937細(xì)胞凋亡和抑制增殖。CI-1040顯著增加PUMA mRNA和蛋白水平。通過(guò)PUMA siRNA轉(zhuǎn)染敲低PUMA，可以抑制CI-1040誘導(dǎo)的U-937細(xì)胞凋亡和增殖抑制[3]。
體內(nèi)活性	處理PD 184352（150 mg/kg，i.p. 或 p.o.）后1小時(shí)和6小時(shí)切除了腫瘤。無(wú)論通過(guò)何種給藥方式，PD 184352處理至少6小時(shí)內(nèi)完全抑制了MAPK磷酸化。MAPK磷酸化在給藥后12小時(shí)恢復(fù)，并在24小時(shí)達(dá)到對(duì)照水平[1]。體內(nèi)，MEK抑制劑CI-1040的系統(tǒng)給藥將腺瘤形成減少至三分之一，并顯著恢復(fù)了肺結(jié)構(gòu)。CL-1040處理的小鼠肺細(xì)胞的增殖率降低，對(duì)肺泡細(xì)胞的分化沒有明顯影響[4]。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 12 mg/mL (25 mM) DMSO : 47.9 mg/mL (100 mM)
關(guān)鍵字	MEK \| Inhibitor \| MAP2K \| Apoptosis \| PD184352 \| MAPKK \| CI 1040 \| PD-184352 \| Mitogen-activated protein kinase kinase \| CI1040 \| inhibit \| CI-1040
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相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 高選擇性抑制劑庫(kù) \| 藥物功能重定位化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 疼痛相關(guān)化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： PD 184352|TargetMol

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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)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于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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