PF-670462
PF-670462
CAS: 950912-80-8
Molecular Formula: C19H20FN5.2HCl
PF-670462 - Names and Identifiers
PF-670462 - Physico-chemical Properties
| Molecular Formula | C19H20FN5.2HCl |
| Molar Mass | 410 |
| Melting Point | >178°C (dec.) |
| Solubility | DMSO: 32 mg/mL( < 1 mg/ml refers to the product slightly soluble or insoluble) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| Use | PF-670462 is a potent, selective inhibitor of casein kinase (CKIε/CKIδ) with IC50 values of 7.7 nM and 14 nM, respectively. |
| In vitro study | 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. |
| In vivo study | 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. |
PF-670462 - Risk and Safety
| WGK Germany | 3 |
PF-670462 - Reference
| Reference Show more | 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. |
PF-670462 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
PF-670462 - Reference Information
| biological activity | PF-670462 are effective, selective CK1ε and CK1δ inhibitors with IC50 of 90 nM and 13 nM respectively. |
| target | TargetValue CK1δ (Cell-free say) 13 nM CK1ε (Cell-free say) 90 nM |
| Target | Value |
| CK1δ (Cell-free assay) | 13 nM |
| CK1ε (Cell-free assay) | 90 nM |
| in vitro study | 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 show less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC 50 s of 150 nM and 190 nM, respectively. PF-670462 also cause a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC 50 of 290±39 nM in CKIε-transferred COS7 cells. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC 50 of 17 nM. PF-670462 (1 μ m) 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. |
| in vivo study | pf -670462 (50 mg/kg, s.c.) produces robust phase remains persistent, and the activity, 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 delay 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. |
| use | PF 670462 is a potent and selective casein kinase(CK1ε) and CK1δ inhibitor. PF 670462 has been shown to inhibit PER protein nuclear translocation causing phase shifts in circadian rhythms. PF 6704 62 attenuates methamphetamine-stimulated locomotion in vivo. |
Last Update：2024-04-09 20:48:19
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Mobile: +86-18621343501
QQ: 2881950922
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Tel: 609-228-6898
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