化合物 Torkinib|T2414|TargetMol

價(jià)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	2025-03-12

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產(chǎn)品詳情

中文名稱(chēng):化合物 Torkinib	英文名稱(chēng):Torkinib
CAS:1092351-67-1	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/Shipping at ambient temperature.
純度規(guī)格: 99.23%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T2414

Product Introduction

Bioactivity

名稱(chēng)	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(xì)胞實(shí)驗(yàn)	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(shí)驗(yàn)	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(dòng)物實(shí)驗(yàn)	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(duì)其他PI3-K家族成員的活性較低。通過(guò)對(duì)219種蛋白激酶的測(cè)試，顯示出相對(duì)于蛋白質(zhì)激酶組的顯著選擇性。在BT549細(xì)胞中，PP242抑制了Akt的磷酸化，mTOR底物p70S6K及其下游靶點(diǎn)S6[1]的磷酸化。PP242以低納摩爾濃度顯著抑制生長(zhǎng)（>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(xì)胞系中表現(xiàn)出更強(qiáng)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(fù)擔(dān)。在一項(xiàng)長(zhǎng)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(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 55 mg/mL (178.37 mM), Sonication is recommended.
關(guān)鍵字	Torkinib \| PP-242 \| PP242 \| p110δ \| mTORC2 \| mTORC1 \| mTOR \| Mitophagy \| Mitochondrial Autophagy \| Mammalian target of Rapamycin \| Inhibitor \| inhibit \| Autophagy \| Apoptosis
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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) \| 抗癌細(xì)胞代謝庫(kù) \| 氧化還原化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗糖尿病庫(kù) \| 抗衰老化合物庫(kù) \| HIF-1化合物庫(kù) \| 癌細(xì)胞分化化合物庫(kù) \| 血液病分子庫(kù) \| 免疫/炎癥分子化合物庫(kù)

關(guān)鍵字： PP 242|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(zhuān)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(xiāo)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(guò)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(guò)五百家學(xué)校和各類(lèi)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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