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445821 Meriolin 3 - CAS 954143-48-7 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
954143-48-7C₁₂H₁₁N₅O

Products

Catalog NumberPackaging Qty/Pack
445821-5MG Plastic ampoule 5 mg
Description
OverviewA cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit the kinase activity of CDK9/cyclin T, CDK2/cyclin A, CDK1/cyclin B, CDK5/p25 (IC50 = 6, 11, 170, 170 nM, respectively), DYRK1A, CKIδ/ε, GSK-3α/β (IC50 = 29, 200, and 230 nM, respectively), as well as CDK3/cyclin E, CDK4/cyclin D1, CDK6/cyclin D1, CDK7/cyclin H, and FLT3 (IC50 <400 nM), while showing much reduced activity agasint 21 other kinases (IC50 >1 µM). Shown to effectively inhibit cellular CDK substrates phosphorylation and induce apoptosis in SH-SY5Y neuroblastoma cultures (Effective conc. 0.3 to 1 µM) in vitro and retard A4573- and LS174T-derived tumor growths in mice in vivo (1 to 5 mg/kg/day, i.p.). Cell viability tests reveal that Meriolin 3 selectively affects the viability of a panel of 8 cancer lines (IC50 ≤380 nM) in comparison to normal human foreskin fibroblasts (IC50 = 8 µM).
Catalogue Number445821
Brand Family Calbiochem®
Synonyms3-((2-Amino)pyrimidin-4-yl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine, Cdk7 Inhibitor VI
References
ReferencesEchalier, A., et al. 2008. J. Med. Chem. 51, 737.
Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.
Product Information
CAS number954143-48-7
FormYellow solid
Hill FormulaC₁₂H₁₁N₅O
Chemical formulaC₁₂H₁₁N₅O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% 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 Ambient Temperature Only
Toxicity Regulatory Review
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 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Identification Number
Catalog Number GTIN
445821-5MG4055977204582

Documentation

Meriolin 3 - CAS 954143-48-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Meriolin 3 - CAS 954143-48-7 - Calbiochem Certificates of Analysis

TitleLot Number
445821

References

Reference overview
Echalier, A., et al. 2008. J. Med. Chem. 51, 737.
Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.
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.

Revision13-April-2011 RFH
Synonyms3-((2-Amino)pyrimidin-4-yl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine, Cdk7 Inhibitor VI
DescriptionA cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit the kinase activity of CDK9/cyclin T, CDK2/cyclin A, CDK1/cyclin B, CDK5/p25 (IC50 = 6, 11, 170, 170 nM, respectively), DYRK1A, CKIδ/ε, GSK-3α/β (IC50 = 29, 200, and 230 nM, respectively), as well as CDK3/cyclin E, CDK4/cyclin D1, CDK6/cyclin D1, CDK7/cyclin H, and FLT3 (IC50 <400 nM), while showing much reduced activity agasint 21 other kinases (IC50 >1 µM). Shown to effectively inhibit cellular CDK substrates phosphorylation and induce apoptosis in SH-SY5Y neuroblastoma cultures (Effective conc. 0.3 to 1 µM) in vitro and retard A4573- and LS174T-derived tumor growths in mice in vivo (1 to 5 mg/kg/day, i.p.). Cell viability tests reveal that Meriolin 3 selectively affects the viability of a panel of 8 cancer lines (IC50 ≤380 nM) in comparison to normal human foreskin fibroblasts (IC50 = 8 µM).
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number954143-48-7
Chemical formulaC₁₂H₁₁N₅O
Structure formulaStructure formula
Purity≥95% 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 3 months at -20°C.
Toxicity Regulatory Review
ReferencesEchalier, A., et al. 2008. J. Med. Chem. 51, 737.
Bettayeb, K., et al. 2007. Cancer Res. 67, 8325.