445821
Meriolin 3
A cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit kinase activity.
Synonym(s):
Meriolin 3, 3-((2-Amino)pyrimidin-4-yl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine, Cdk7 Inhibitor VI
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About This Item
Empirical Formula (Hill Notation):
C12H11N5O
CAS Number:
Molecular Weight:
241.25
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C12H11N5O/c1-18-9-3-5-14-11-10(9)7(6-16-11)8-2-4-15-12(13)17-8/h2-6H,1H3,(H,14,16)(H2,13,15,17)
InChI key
GGEWEQJWGGJUHO-UHFFFAOYSA-N
General description
A 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).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Echalier, A., et al. 2008. J. Med. Chem.51, 737.
Bettayeb, K., et al. 2007. Cancer Res.67, 8325.
Bettayeb, K., et al. 2007. Cancer Res.67, 8325.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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