AD80
作者：齐岳
发布时间：2023-09-07
09:26:04
点击数：
产品名称：AD80
产品描述：
| 产品描述 | AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity. |
| 靶点活性 | RET V804L:0.6 nM, RET V804M:0.4 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 | 473.44 |
| 分子式 | C22H19F4N7O |
| CAS No. | 1384071-99-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 150 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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