(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
APILIMOD(APILIMOD)
CAS: 541550-19-0
化学式: C23H26N6O2
| 中文名 | APILIMOD |
| 英文名 | APILIMOD |
| 别名 | 阿吡莫德 阿匹莫德 4-(6-(2-(3-甲基亚苄基)肼基)-2-(2-(吡啶-2-基)乙氧基)嘧啶-4-基)吗啉 |
| 英文别名 | Sta5326 Sta-5326 APILIMOD Sta 5326 APILIMODUM ApiliMod(STA5326) 3-Methylbenzaldehyde 2-[6-(4-Morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyriMidinyl]hydrazone (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine |
| CAS | 541550-19-0 |
| 化学式 | C23H26N6O2 |
| 分子量 | 418.49 |
| 密度 | 1.24 |
| 沸点 | 655.1±65.0 °C(Predicted) |
| 溶解度 | 溶于DMSO (>25 mg/ml) |
| 酸度系数 | 12.56±0.10(Predicted) |
| 存储条件 | -20°C |
| 稳定性 | 稳定1年的供应。DMSO中的溶液可以在-20 °C下储存长达3个月。 |
| 外观 | 固体 |
| 颜色 | White |
| 靶点 | IL-12 IL-23 PIKfyve |
| 参考资料 展开查看 | 1: Cai X, Xu Y, Kim YM, Loureiro J, Huang Q. PIKfyve, a class III lipid kinase, is required for TLR-induced type I IFN production via modulation of ATF3. J Immunol. 2014 Apr 1;192(7):3383-9. doi: 10.4049/jimmunol.1302411. Epub 2014 Mar 5. PubMed PMID: 24600036. 2: Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M, Rondeau JM, Fazal AN, Wilson CJ, Myer V, Joberty G, Bouwmeester T, Labow MA, Finan PM, Porter JA, Ploegh HL, Baird D, De Camilli P, Tallarico JA, Huang Q. PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling. Chem Biol. 2013 Jul 25;20(7):912-21. doi: 10.1016/j.chembiol.2013.05.010. PubMed PMID: 23890009. 3: Baird AM, Dockry E, Daly A, Stack E, Doherty DG, O'Byrne KJ, Gray SG. IL-23R is Epigenetically Regulated and Modulated by Chemotherapy in Non-Small Cell Lung Cancer. Front Oncol. 2013 Jun 19;3:162. doi: 10.3389/fonc.2013.00162. eCollection 2013. PubMed PMID: 23802098; PubMed Central PMCID: PMC3685824. 4: Wada Y, Cardinale I, Khatcherian A, Chu J, Kantor AB, Gottlieb AB, Tatsuta N, Jacobson E, Barsoum J, Krueger JG. Apilimod inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis. PLoS One. 2012;7(4):e35069. doi: 10.1371/journal.pone.0035069. Epub 2012 Apr 6. PubMed PMID: 22493730; PubMed Central PMCID: PMC3320873. |
(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.389 ml | 11.947 ml | 23.895 ml |
| 5 mM | 0.478 ml | 2.389 ml | 4.779 ml |
| 10 mM | 0.239 ml | 1.195 ml | 2.389 ml |
| 5 mM | 0.048 ml | 0.239 ml | 0.478 ml |
最后更新：2024-01-02 23:10:35
(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine - 细胞实验
Cervical lymph node cells obtained from immunized mice on day 18 (2×105 cells/well) arecultured in 0.2 mL RPMI 1640 containing 10 mM HEPES, 0.1 mM nonessential amino acid, 1 mM sodium pyruvate, 100 U/mL penicillin, 100 μg/mL streptomycin, 1×10-5 M 2-mercaptoethanol, 10% FCS, and 10 μg/mL IRBP1-20. For cytokine assay, supernatants are collected after 72 hours and analysed for IFN-γ, IL-4 and IL-17 by quantitative capture ELISA using quantikine ELISA kits and mouse IL-17 ELISA Ready-SET-Go kits. Cell proliferation is evaluated using a cell proliferation assay.
最后更新：2023-08-16 21:32:38
(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine - 动物实验
In most experiments, 5 mg/kg or 20 mg/kg Apilimod or vehicle only (0.5% carboxyl methyl cellulose) is orally administered once a day for six days a week from day 0 to day 14 after immunization. In the effector phase experiments, 20 mg/kg Apilimod or vehicle is orally administered once a day, from day 9 to day 14 after immunization.
最后更新：2023-08-16 21:32:38
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