化合物 Torkinib|T2414|TargetMol

價格	￥169	￥359	￥596
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 Torkinib	英文名稱:Torkinib
CAS:1092351-67-1	品牌: TargetMol
產(chǎn)地: 美國	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: 99.23%	產(chǎn)品類別: 抑制劑
貨號: T2414

Product Introduction

Bioactivity

名稱	Torkinib
描述	Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
細胞實驗	Cells were seeded in triplicate wells of 96-well flat bottom culture plates for 48 hr in the presence of increasing concentrations of indicated inhibitors. Cell viability and median-effect dose affecting growth (GIC50) was determined using the MTS assay. Absorbance values (490 nm) were normalized to controls and expressed as %MTS conversion. Wells lacking cells but with MTS added was used as the zero value when normalizing. For drug combination experiments, a range of fixed ratios of inhibitors was used to assess synergy using the combination index (CI) with CalcuSyn software according to the median-effect method as previously described. For proliferation experiments with PC-3, SKOV3, 786-O, and U87 cells, the CellTiter-Glo Luminescent reagent was used following the manufacturer's instructions. Quantitation was performed as mentioned above [2].
激酶實驗	Purified kinase domains were incubated with inhibitors at 2- or 4-fold dilutions over a concentration range of 50 - 0.001 μM or with vehicle (0.1% DMSO) in the presence of 10 μM ATP, 2.5 μCi of γ-32P-ATP and substrate. Reactions were terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane was then washed 5–6 times to remove unbound radioactivity and dried. Transferred radioactivity was quantitated by phosphorimaging and IC50 values were calculated by fitting the data to a sigmoidal doseresponse using Prism software [1].
動物實驗	Drugs were prepared in 100 μl of vehicle containing 20% DMSO, 40% PEG-400, and 40% saline. Six-wk-old male C57BL/6 mice were fasted overnight prior to drug treatment. PP242 (0.4 mg), rapamycin (0.1 mg), or vehicle alone was injected IP. After 30 min for the rapamycin-treated mouse or 10 min for the PP242 and vehicle-treated mice, 250 mU of insulin in 100 μl of saline was injected IP. 15 min after the insulin injection, the mice were killed by CO2 asphyxiation followed by cervical dislocation. Tissues were harvested and frozen on liquid nitrogen in 200 μl of cap lysis buffer. The frozen tissue was thawed on ice, manually disrupted with a mortar and pestle, and then further processed with a micro tissue-homogenizer. The protein concentration of the cleared lysate was measured by Bradford assay and 5–10 μg of protein was analyzed by Western blot as described above [3].
體外活性	Torkinib（PP242）有效抑制了mTOR（IC50：8 nM），但對其他PI3-K家族成員的活性較低。通過對219種蛋白激酶的測試，顯示出相對于蛋白質(zhì)激酶組的顯著選擇性。在BT549細胞中，PP242抑制了Akt的磷酸化，mTOR底物p70S6K及其下游靶點S6[1]的磷酸化。PP242以低納摩爾濃度顯著抑制生長（>90%，GI50：12 nM）。與雷帕霉素相比，PP242在攜帶PI3K功能增益或PTEN功能喪失的固體腫瘤細胞系中表現(xiàn)出更強的抗增殖效力[2]。
體內(nèi)活性	在鼠p190模型中，短期口服Torkinib以劑量依賴的方式顯著降低了脾臟和骨髓中的白血病負擔。在一項長期生存研究中，口服Torkinib（30和60 mg/kg）顯著推遲了白血病的發(fā)病[2]。在脂肪和肝臟中，Torkinib能完全抑制Akt在S473和T308的磷酸化。令人驚訝的是，在骨骼肌中，Torkinib只能部分抑制Akt的磷酸化，并且在抑制T308的磷酸化方面比S473更有效，盡管它能完全抑制4EBP1和S6的磷酸化[3]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (178.37 mM)
關(guān)鍵字	Mitophagy \| Autophagy \| Mammalian target of Rapamycin \| mTOR \| PP-242 \| Torkinib \| Apoptosis \| PP242 \| inhibit \| Mitochondrial Autophagy \| Inhibitor
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相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 抗胰腺癌化合物庫 \| 激酶抑制劑庫 \| 神經(jīng)再生化合物庫 \| 細胞凋亡化合物庫 \| 抗衰老化合物庫 \| 抗肥胖化合物庫 \| 抗氧化化合物庫

關(guān)鍵字： PP 242|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，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。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，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)過在中國市場五年的精心耕耘，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

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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