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218719 Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem

218719
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1188296-52-7C₁₇H₁₈ClN₅O₂

Products

Catalogue NumberPackaging Qty/Pack
218719-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
Catalogue Number218719
Brand Family Calbiochem®
Synonyms3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
References
ReferencesMeng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
Product Information
CAS number1188296-52-7
FormBeige solid
Hill FormulaC₁₇H₁₈ClN₅O₂
Chemical formulaC₁₇H₁₈ClN₅O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
218719-5MG 04055977218947

Documentation

Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem Certificates of Analysis

TitleLot Number
218719

References

Reference overview
Meng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision20-July-2012 JSW
Synonyms3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
DescriptionA cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
FormBeige solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1188296-52-7
Chemical formulaC₁₇H₁₈ClN₅O₂
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesMeng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.