Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AD80 是多激酶抑制剂,可抑制 RET、RAF、SRC 和 S6K,并大大降低 mTOR 活性。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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