化合物 PD0325901|T6189

價(jià)格	￥189	￥428	￥738
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:化合物 PD0325901	英文名稱:Mirdametinib
CAS:391210-10-9	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: 99.63%	產(chǎn)品類別: 抑制劑
貨號(hào): T6189

Product Introduction

Bioactivity

名稱	Mirdametinib
描述	Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.
細(xì)胞實(shí)驗(yàn)	A cell death detection enzyme-linked immunosorbent assay was used per the manufacturer's instructions. Briefly, 4 × 10^4 cells were plated in 24-well plates in triplicate the day before treatment. PTC cells were treated with 0.1 μmol/L PD0325901 for 96 hours. Cells treated with 1 μmol/L staurosporine served as positive controls for apoptosis. At the end of treatment, cells were lysed using the lysis buffer provided in the kit for 30 minutes at room temperature and then centrifuged in 24-well plates. Lysates (20 μL of supernatant) were transferred to streptavidin-coated wells and incubated for 2 hours at room temperature with two antibodies (biotin-labeled anti-histone antibody and peroxidase-conjugated anti-DNA antibody). After the wells were washed three times, the samples were incubated with peroxidase substrate (ABTS) and the amount of colored product was determined spectrophotometrically at 405 nm. The background was measured at 490 nm [2].
激酶實(shí)驗(yàn)	Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of a glutathione S-transferase fusion protein containing p44MAP kinase (GST-MAPK) and a glutathione S-transferase protein containing p45MEK (GST-MEK). The assay solution contained 20 mM HEPES, pH 7.4, 10 mM MgCl2, 1 mM MnCl2, 1 mM EGTA, 50 mM [γ-32P]ATP, 10 mg GST-MEK, 0.5 mg GST-MAPK and 40 mg MBP in a final volume of 100 mL. Reactions are stopped after 20 minutes by addition of trichloroacetic acid and filtered through a GF/C filter mat. 32P retained on the filter mat is determined using a 1205 Betaplate [1].
動(dòng)物實(shí)驗(yàn)	Athymic Ncr-nu/nu mice were obtained from the National Cancer Institute at ages 6 to 8 weeks and housed for at least 1 week after arrival. Mice (10–14 per group) were anesthetized s.c. with a cocktail (100 μL/10 g body weight of 10 mg/mL ketamine and 1 mg/mL xylazine). K2 and TPC-1 cells stably infected with a retrovirus expressing luciferase (5 × 105 cells in 5 μL RPMI1640 medium) were inoculated into the thyroid gland, and the mice were monitored weekly for tumor growth by Xenogen (IVIS 200 imaging system) using Living Image 3.0 software. One week after inoculation, PD0325901 was dissolved in 80 mmol/L citric buffer (pH 7) by sonication and given to mice daily by oral gavage (20–25 mg/kg) for 3 weeks (5 consecutive days/week). Mice were sacrificed only due to tumor burden or loss of 20% of body weight. Tumor sizes were measured with calipers and tumor volume (V) was calculated by the formula (V = length × width × depth). Control mice were given 80 mmol/L citric buffer (pH 7) alone. All in vivo experiments were done at least twice [2].
體外活性	方法：11 種人黑色素瘤細(xì)胞系上用 Mirdametinib (0.1-1000 nM) 處理 72 h，使用 trypan blue exclusion test 檢測(cè)細(xì)胞數(shù)。結(jié)果：Mirdametinib (IC50=20-50 nM) 有效抑制具有 BRAF 突變 (M14/A375P/A375M/A375SM/ME10538/ME4686/JR8) 或不具有 BRAF 突變 (ME4405/ME13923) 的人黑色素瘤細(xì)胞系的生長(zhǎng)。ME1007 和 ME8959均具有野生型 BRAF，對(duì) Mirdametinib介導(dǎo)的生長(zhǎng)抑制的抗性略高 (IC50≥100 nM)。[1] 方法：乳頭狀甲狀腺癌 (PTC) 細(xì)胞系 K2 和 TPC-1 用 Mirdametinib (0.1-1000 nmol/L) 處理 1-96 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Mirdametinib 可以有效抑制多種 PTC 細(xì)胞系中 ERK1/2 的磷酸化。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Mirdametinib (20-25 mg/kg，80 mmol/L citric buffer (pH 7)) 灌胃給藥給攜帶 PTC 腫瘤 K2 或 TPC-1 的 Athymic Ncr-nu/nu 小鼠，每周五次，持續(xù)三周。結(jié)果：Mirdametinib 在接種攜帶 BRAF 突變的 PTC 細(xì)胞 K2 的小鼠中完全抑制腫瘤生長(zhǎng)，并且在接種攜帶 RET/PTC1 重排的 PTC 細(xì)胞 TPC-1 的小鼠中顯著降低腫瘤生長(zhǎng)。[2] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Mirdametinib (1.6-25 mg/kg，0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in water) 口服給藥給攜帶小鼠結(jié)直腸癌腫瘤 CT26 的小鼠，每天一次，持續(xù)十四天。結(jié)果：Mirdametinib 顯著抑制腫瘤中的 pERK 水平。[3]
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	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.37 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : Insoluble DMSO : 50 mg/mL (103.69 mM)
關(guān)鍵字	PD 0325901 \| MAPKK \| Mitogen-activated protein kinase kinase \| Apoptosis \| MEK \| PD-0325901 \| Autophagy \| inhibit \| MAP2K \| PD-325901 \| Inhibitor \| PD 325901 \| Mirdametinib
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相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 高選擇性抑制劑庫 \| 抗衰老化合物庫 \| 疼痛相關(guān)化合物庫 \| 酪氨酸激酶分子庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： PD325901|||PD0325901|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

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