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[5-amino-8-[4-(1-methylpyrazol-4-yl)phenyl]-1,6-naphthyridin-2-yl]-(3-methoxyazetidin-1-yl)methanone , CAS No.A609294, Inhibitor of cyclin dependent kinase 19;Inhibitor of cyclin dependent kinase 8

  • Moligand™
Item Number
A609294
Grouped product items
SKUSizeAvailabilityPrice Qty
A609294-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,000.90
A609294-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,000.90

Basic Description

Synonymscompound 51
Specifications & PurityMoligand™
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of cyclin dependent kinase 19;Inhibitor of cyclin dependent kinase 8

Associated Targets

CDK8 Tchem Cyclin-dependent kinase 8 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CCNC Tbio Cyclin-C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK19 Tchem Cyclin-dependent kinase 19 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AOX1 Tchem Aldehyde oxidase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name [5-amino-8-[4-(1-methylpyrazol-4-yl)phenyl]-1,6-naphthyridin-2-yl]-(3-methoxyazetidin-1-yl)methanone
INCHI InChI=1S/C23H22N6O2/c1-28-11-16(9-26-28)14-3-5-15(6-4-14)19-10-25-22(24)18-7-8-20(27-21(18)19)23(30)29-12-17(13-29)31-2/h3-11,17H,12-13H2,1-2H3,(H2,24,25)
InChi Key OJIQEAIHEGJBFE-UHFFFAOYSA-N
Canonical SMILES COC1CN(C1)C(=O)c1ccc2c(n1)c(cnc2N)c1ccc(cc1)c1cnn(c1)C
Isomeric SMILES CN1C=C(C=N1)C2=CC=C(C=C2)C3=CN=C(C4=C3N=C(C=C4)C(=O)N5CC(C5)OC)N
PubChem CID 118660867

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References

1. Firestein R, Bass AJ, Kim SY, Dunn IF, Silver SJ, Guney I, Freed E, Ligon AH, Vena N, Ogino S et al..  (2008)  CDK8 is a colorectal cancer oncogene that regulates beta-catenin activity..  Nature,  455  (7212): (547-51).  [PMID:18794900]
2. Kapoor A, Goldberg MS, Cumberland LK, Ratnakumar K, Segura MF, Emanuel PO, Menendez S, Vardabasso C, Leroy G, Vidal CI et al..  (2010)  The histone variant macroH2A suppresses melanoma progression through regulation of CDK8..  Nature,  468  (7327): (1105-9).  [PMID:21179167]
3. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al..  (2016)  2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19..  ACS Med Chem Lett,  (6): (573-8).  [PMID:27326329]

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