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AD80

AD80

产品编号 T4301   CAS 1384071-99-1

AD80 是多激酶抑制剂,可抑制 RET、RAFSRC 和 S6K,并大大降低 mTOR 活性。

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AD80 Chemical Structure
AD80, CAS 1384071-99-1
规格 价格/CNY 货期 数量
1 mg ¥ 385 现货
5 mg ¥ 949 现货
10 mg ¥ 1,520 现货
25 mg ¥ 2,970 现货
50 mg ¥ 4,390 现货
100 mg ¥ 6,280 现货
500 mg ¥ 12,800 现货
1 mL * 10 mM (in DMSO) ¥ 991 现货
产品目录号及名称: AD80 (T4301)
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纯度: 100%
纯度: 99.9%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
靶点活性 RET V804M:0.4 nM, RET V804L:0.6 nM
体外活性 AD80 and AD81 inhibits RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58.AD80 is optimal for Ras–Erk pathway inhibition. AD80 is a polypharmacological agent with an optimal balance of activity against Ret, Raf, Src, Tor and S6K that show high efficacy with very low toxicity. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis. AD80 coordinately inhibits S6K1 together with the TAM family tyrosine kinase AXL.AD80 avoides S6K1 phosphorylation and mTOR co-association, resulting in durable suppression of S6K1-induced signaling and protein synthesis.
体内活性 AD80 rescues 50% of mice transplanted with PTEN-deficient leukemia cells. Oral administration of either AD80 or AD81 results in a notable 70-90% of animals developing to adulthood in Drosophila ptc>dRetMEN2Bmodel, a considerable improvement over the efficacy observed with AD57. AD80 also promotes enhanced tumour growth inhibition and reduces body-weight modulation relative to vandetanib in a mouse xenograft model.
细胞实验 MZ-CRC-1 (MEN2B) and TT (MEN2A) cells are treated with AD80 (0.2 nM to 20 μM) for 7 days and cell viability is quantitated by MTT assay.
动物实验 Mice showing established growing tumors are separated into vehicle or drug treatment groups. A similar range of tumor sizes is selected for each experiment (vehicle vs AD57; vehicle vs AD80 vs Vandetanib). Vehicle, AD57 (20 mg/kg), AD80 (30 mg/kg), or Vandetanib (50 mg/kg) are administered by oral gavage (PO; per os or by mouth) once daily, five times a week. Tumor and body weight measurements are performed 3 times a week.
分子量 473.43
分子式 C22H19F4N7O
CAS No. 1384071-99-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 150 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Dar AC, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology.Nature. 2012 Jun 6;486(7401):80-4. 2. Liu H, et al. Pharmacologic Targeting of S6K1 in PTEN-Deficient Neoplasia.Cell Rep. 2017 Feb 28;18(9):2088-2095. 3. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis[J]. Investigational New Drugs. 2021: 1-11.

文献引用

1. de Almeida L C, Carlos J A E G, Rezende-Teixeira P, et al. AD80, a multikinase inhibitor, as a potential drug candidate for colorectal cancer therapy. Life Sciences. 2022: 120911. 2. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis. Investigational New Drugs. 2021 Aug;39(4):1139-1149. doi: 10.1007/s10637-021-01066-w. Epub 2021 Jan 21. 3. Carlos J A E G, Lima K, Costa-Lotufo L V, et al. AD80, a multikinase inhibitor, exhibits antineoplastic effects in acute leukemia cellular models targeting the PI3K/STMN1 axis. Investigational New Drugs. 2021 Aug;39(4):1139-1149. doi: 10.1007/s10637-021-01066-w. Epub 2021 Jan 21. 4. Lima K, de Miranda L B L, Del Milagro Bernabe Garnique A, et al.The Multikinase Inhibitor AD80 Induces Mitotic Catastrophe and Autophagy in Pancreatic Cancer Cells.Cancers.2023, 15(15): 3866.
Raf inhibitor 3 Lifirafenib SOS1-IN-11 PLX-4720 B-Raf IN 16 BMS-214662 RAF709 Regorafenib monohydrate

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 HIF-1化合物库 细胞凋亡化合物库 激酶抑制剂库 抗肥胖化合物库 抗胰腺癌化合物库 干细胞分化化合物库 MAPK 抑制剂库 氧化还原化合物库 抗肺癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AD80 1384071-99-1 Angiogenesis Apoptosis MAPK PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Raf c-RET Src S6 Kinase AD 80 Inhibitor inhibit Raf kinases AD-80 Ribosomal S6 Kinase (RSK) S6K RET inhibitor

 

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