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RG-1530 , Serine/threonine-protein kinase PLK4 inhibitor, CAS No.R613169, Serine/threonine-protein kinase PLK4 inhibitor

  • Moligand™
Item Number
R613169
Grouped product items
SKUSizeAvailabilityPrice Qty
R613169-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,334.90
R613169-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,001.90

Basic Description

Synonyms882531-87-5|R-1530|R1530|RG-1530|5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepine|XQJ55R5PPQ|CID 11610113|CHEMBL1980391|5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepin
Specifications & PurityMoligand™
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionSerine/threonine-protein kinase PLK4 inhibitor

Associated Targets

CNBD1 Tdark Cyclic nucleotide-binding domain-containing protein 1 0 Activities

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

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

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

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

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

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

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

DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B 0 Activities

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

EGFR Tclin Epidermal growth factor receptor 0 Activities

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

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

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

CDK4 Tclin Cyclin-dependent kinase 4 0 Activities

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

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

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

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

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

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

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

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

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

HDAC6 Tclin Histone deacetylase 6 0 Activities

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

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

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

FGFR1 Tclin Fibroblast growth factor receptor 1 1 Activities

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

FGFR3 Tclin Fibroblast growth factor receptor 3 1 Activities

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

MET Tclin Hepatocyte growth factor receptor 0 Activities

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

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

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

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

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

PLK4 Tchem Serine/threonine-protein kinase PLK4 2 Activities

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

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

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

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

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

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

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

PIM3 Tchem Serine/threonine-protein kinase pim-3 0 Activities

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

PRKG2 Tchem cGMP-dependent protein kinase 2 0 Activities

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

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 0 Activities

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

MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 0 Activities

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

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

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

AURKA Tchem Aurora kinase A 1 Activities

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

FLT1 Tclin Vascular endothelial growth factor receptor 1 0 Activities

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

KDR Tclin Vascular endothelial growth factor receptor 2 2 Activities

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

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

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

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

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

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

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

ALK Tclin ALK tyrosine kinase receptor 0 Activities

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

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

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

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

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

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

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

CHEK2 Tchem Serine/threonine-protein kinase Chk2 1 Activities

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

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

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

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

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

GSK3B Tclin Glycogen synthase kinase-3 beta 1 Activities

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

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

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

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

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

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

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

JAK2 Tclin Tyrosine-protein kinase JAK2 0 Activities

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

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

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

Names and Identifiers

IUPAC Name 5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-2,10-dihydropyrazolo[3,4-b][1,4]benzodiazepine
INCHI InChI=1S/C18H14ClFN4O/c1-9-16-18(24-23-9)21-14-8-15(25-2)13(20)7-11(14)17(22-16)10-5-3-4-6-12(10)19/h3-8H,1-2H3,(H2,21,23,24)
InChi Key UOVCGJXDGOGOCZ-UHFFFAOYSA-N
Canonical SMILES COc1cc2[nH]c3n[nH]c(c3nc(c2cc1F)c1ccccc1Cl)C
Isomeric SMILES CC1=C2C(=NN1)NC3=CC(=C(C=C3C(=N2)C4=CC=CC=C4Cl)F)OC
PubChem CID 135398512

Certificates

Certificate of Analysis(COA)

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Related Documents

References

1. Tovar C, Higgins B, Deo D, Kolinsky K, Liu JJ, Heimbrook DC, Vassilev LT.  (2010)  Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy..  Cell Cycle,  (16): (3364-75).  [PMID:20814247]
2. Kolinsky K, Tovar C, Zhang YE, Railkar A, Yang H, Carvajal D, Nevins T, Geng W, Linn M, Packman K et al..  (2011)  Preclinical evaluation of the novel multi-targeted agent R1530..  Cancer Chemother Pharmacol,  68  (6): (1585-94).  [PMID:21553286]
3. Laufer R, Forrest B, Li SW, Liu Y, Sampson P, Edwards L, Lang Y, Awrey DE, Mao G, Plotnikova O et al..  (2013)  The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents..  J Med Chem,  56  (15): (6069-87).  [PMID:23829549]
4. Liu JJ, Higgins B, Ju G, Kolinsky K, Luk KC, Packman K, Pizzolato G, Ren Y, Thakkar K, Tovar C et al..  (2013)  Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors..  ACS Med Chem Lett,  (2): (259-63).  [PMID:24900658]

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