| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 491.9 |
| Formula | C22H20F3N7O·HCl |
| Solubility | ≤5mg/ml in ethanol;10mg/ml in DMSO;14mg/ml in dimethyl formamide |
| Chemical Name | N-[4-[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]-urea, monohydrochloride |
| Canonical SMILES | CC(C)N1C2=NC=NC(N)=C2C(C3=CC=C(NC(NC4=CC(C(F)(F)F)=CC=C4)=O)C=C3)=N1.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 2 nM: blocks the receptor tyrosine kinase RET in Drosophila.
AD57, as a polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer. AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numerous other kinases, and interferes with kinases downstream of RET, including Raf, Src, and S6K, providing further efficacy in preventing signaling leading to invasion, proliferation, and metabolism related to cancer. Tyrosine kinase RET is probably sufficient to initiate a series of transformation events including medullary thyroid carcinoma, multiple endocrine neoplasias type 2A (MEN2A) and 2B (MEN2B).
In vitro: AD57 was demonstrated to be able to inhibit tyrosine kinase RET. But the efficacy of AD57 did not correlate solely with the blockade of RET, suggesting that the targeting of additional kinases is necessary for its biological efficacy. AD57 potently dampened the pathway-related human kinases B-Raf, mTOR, S6K, and Src [1].
In vivo: Male nu nu mice, injected subcutaneously with MEN2A cell lines, were administered AD57 (20 mg/kg) by oral gavage (per os) once daily, five times a week. AD57 inhibited the activity of relevant target kinases at 1 μM compared with the vehicle-treated nude mice transplanted with MEN2A cells [1].
Reference:
[1]. Dar, A., Das, T., Shokat, K., & Cagan, R. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012; 486(7401): 80-84.
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