4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐
PF-670462(PF-670462)
CAS: 950912-80-8
化学式: C19H20FN5.2HCl
| 中文名 | PF-670462 |
| 英文名 | PF-670462 |
| 别名 | 化合物PF670462 PF-670462盐酸盐 CK1Ε抑制剂(PF-670462) 4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 |
| 英文别名 | PF 67046 PF 670462 PF-670462 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine hydrochloride 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinaminedihydrochloride 4-[3-Cyclohexyl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-ylamine dihydrochloride 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine hydrochloride PF670462 |
| CAS | 950912-80-8 |
| 化学式 | C19H20FN5.2HCl |
| 分子量 | 410 |
| InChIKey | PSNKGVAXBSAHCH-UHFFFAOYSA-N |
| 熔点 | >178°C (dec.) |
| 溶解度 | H2O: 可溶物2mg/mL，澄清 (温热) |
| 存储条件 | 2-8°C |
| 外观 | 粉末 |
| 颜色 | white to beige |
| 体外研究 | PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC 50 s of 7.7 nM and 14 nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC 50 s of 150 nM and 190 nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC 50 of 290 ± 39 nM in CKIε-transfected COS7 cells. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC 50 of ∼17 nM. PF-670462 (1 μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100 nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling. |
| 体内研究 | PF-670462 (50 mg/kg, s.c.) produces robust phase delays, and the activity remains persistent, with no discernible correction in the absence of exogenous zeitgebers in rats. PF-670462 (25, 50, and 100 mg/kg, s.c.) induces dose-dependent phase shift. PF-670462 (50 mg/kg; s.c.) significantly phase delays the rhythmic transcription of Bmal1, Per1, Per2 and Nr1d1 in both liver and pancreas by 4.5 ± 1.3 h and 4.5 ± 1.2 h, respectively, 1 day after administration. In the suprachiasmatic nucleus (SCN), the rhythm of Nr1d1 and Dbp mRNA expression is also delayed by 4.2 and 4 h, respectively. |
| WGK Germany | 3 |
| 参考资料 展开查看 | 1: Young EE, Bryant CD, Lee SE, Peng X, Cook B, Nair HK, Dreher KJ, Zhang X, Palmer AA, Chung JM, Mogil JS, Chesler EJ, Lariviere WR. Systems genetic and pharmacological analysis identifies candidate genes underlying mechanosensation in the von Frey test. Genes Brain Behav. 2016 Jul;15(6):604-15. doi: 10.1111/gbb.12302. PubMed PMID: 27231153. 2: Solocinski K, Richards J, All S, Cheng KY, Khundmiri SJ, Gumz ML. Transcriptional regulation of NHE3 and SGLT1 by the circadian clock protein Per1 in proximal tubule cells. Am J Physiol Renal Physiol. 2015 Dec 1;309(11):F933-42. doi: 10.1152/ajprenal.00197.2014. Epub 2015 Sep 16. PubMed PMID: 26377793; PubMed Central PMCID: PMC4669359. 3: Kennaway DJ, Varcoe TJ, Voultsios A, Salkeld MD, Rattanatray L, Boden MJ. Acute inhibition of casein kinase 1δ/ε rapidly delays peripheral clock gene rhythms. Mol Cell Biochem. 2015 Jan;398(1-2):195-206. doi: 10.1007/s11010-014-2219-8. Epub 2014 Sep 23. PubMed PMID: 25245819. 4: Zhang L, Hastings MH, Green EW, Tauber E, Sladek M, Webster SG, Kyriacou CP, Wilcockson DC. Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra. Curr Biol. 2013 Oct 7;23(19):1863-73. doi: 10.1016/j.cub.2013.08.038. Epub 2013 Sep 26. PubMed PMID: 24076244; PubMed Central PMCID: PMC3793863. |
4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.437 ml | 12.186 ml | 24.371 ml |
| 5 mM | 0.487 ml | 2.437 ml | 4.874 ml |
| 10 mM | 0.244 ml | 1.219 ml | 2.437 ml |
| 5 mM | 0.049 ml | 0.244 ml | 0.487 ml |
最后更新：2024-01-02 23:10:35
4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 - 简介
PF-670462是一种有机化合物。它是一种靶向蛋白激酶的抑制剂。
制备PF-670462的方法通常涉及多个有机合成步骤。具体来说，它的合成常从简单的起始原料开始，并通过连续的化学反应步骤来构建目标分子。
在使用该化合物时，需要严格遵守实验室安全操作规程，并采取适当的防护措施，如佩戴手套、护目镜等。
制备PF-670462的方法通常涉及多个有机合成步骤。具体来说，它的合成常从简单的起始原料开始，并通过连续的化学反应步骤来构建目标分子。
在使用该化合物时，需要严格遵守实验室安全操作规程，并采取适当的防护措施，如佩戴手套、护目镜等。
最后更新：2024-04-09 20:48:19
![4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐](http://res.chembk.com/assets/images/structure/312070.gif)
供应商列表
现货供应
产品名: PF-670462 Dihydrochloride 去供应商网站查看 询盘CAS: 950912-80-8
产地: 北京
包装: 盒
规格: IP6780-10mg,10mg
价格: 电话、微信、QQ、邮件
库存: 现询
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 索莱宝直销，欢迎来询
现货供应
产品名: PF-670462盐酸盐 去供应商网站查看 询盘CAS: 950912-80-8
产地: 中国上海
包装: 100mg
规格: 98%
价格: 1827.00
库存: 现货
电话: 400-900-4166
手机: 18017137653
电子邮件: 3007523013@qq.com
QQ: 3007523013
微信: 18017137653
产品描述: 中文名：PF-670462盐酸盐 英文名:PF-670462 CAS:950912-80-8 规格:98% 产地:中国上海
现货供应
产品名: PF-670462 Dihydrochloride 去供应商网站查看 询盘CAS: 950912-80-8
产地: 北京
包装: 盒
规格: IP6780-10mg,10mg
价格: 电话、微信、QQ、邮件
库存: 现询
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 索莱宝直销，欢迎来询
现货供应
产品名: PF-670462盐酸盐 去供应商网站查看 询盘CAS: 950912-80-8
产地: 中国上海
包装: 100mg
规格: 98%
价格: 1827.00
库存: 现货
电话: 400-900-4166
手机: 18017137653
电子邮件: 3007523013@qq.com
QQ: 3007523013
微信: 18017137653
产品描述: 中文名：PF-670462盐酸盐 英文名:PF-670462 CAS:950912-80-8 规格:98% 产地:中国上海
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