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Merck

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:
954143-48-7
Molecular Weight:
241.25
UNSPSC Code:
12352200

Quality Level

100

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)

Storage Class Code

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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