化合物 Torkinib|T2414|TargetMol

Torkinib
1092351-67-1

￥169 1mg 起订

￥359 5mg 起订

￥596 10mg 起订

上海更新日期：2024-09-24

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 Torkinib

英文名称：: Torkinib

CAS号：: 1092351-67-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.23%

产品类别：: 抑制剂

货号：: T2414

Product Introduction

Bioactivity

名称	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).
细胞实验	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].
激酶实验	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].
动物实验	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].
体外活性	Torkinib（PP242）有效抑制了mTOR（IC50：8 nM），但对其他PI3-K家族成员的活性较低。通过对219种蛋白激酶的测试，显示出相对于蛋白质激酶组的显著选择性。在BT549细胞中，PP242抑制了Akt的磷酸化，mTOR底物p70S6K及其下游靶点S6[1]的磷酸化。PP242以低纳摩尔浓度显著抑制生长（>90%，GI50：12 nM）。与雷帕霉素相比，PP242在携带PI3K功能增益或PTEN功能丧失的固体肿瘤细胞系中表现出更强的抗增殖效力[2]。
体内活性	在鼠p190模型中，短期口服Torkinib以剂量依赖的方式显著降低了脾脏和骨髓中的白血病负担。在一项长期生存研究中，口服Torkinib（30和60 mg/kg）显著推迟了白血病的发病[2]。在脂肪和肝脏中，Torkinib能完全抑制Akt在S473和T308的磷酸化。令人惊讶的是，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，尽管它能完全抑制4EBP1和S6的磷酸化[3]。
存储条件	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)
关键字	Mitophagy \| Autophagy \| Mammalian target of Rapamycin \| mTOR \| PP-242 \| Torkinib \| Apoptosis \| PP242 \| inhibit \| Mitochondrial Autophagy \| Inhibitor
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相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗胰腺癌化合物库 \| 激酶抑制剂库 \| 神经再生化合物库 \| 细胞凋亡化合物库 \| 抗衰老化合物库 \| 抗肥胖化合物库 \| 抗氧化化合物库

PP 242|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子