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GSK1070916 - ≥98%, high purity , Serine/threonine-protein kinase Aurora-C inhibitor, CAS No.942918-07-2, Serine/threonine-protein kinase Aurora-C inhibitor

  • Moligand™
  • ≥98%
Item Number
G127938
Grouped product items
SKUSizeAvailabilityPrice Qty
G127938-5mg
5mg
In stock
$116.90
G127938-10mg
10mg
In stock
$195.90
G127938-25mg
25mg
In stock
$441.90
G127938-50mg
50mg
In stock
$521.90
G127938-100mg
100mg
In stock
$913.90

Basic Description

SynonymsGSK1070916|942918-07-2|GSK-1070916|GSK-1070916A|GSK 1070916|3-(4-(4-(2-(3-((dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea|8VLB51V7HO|N'-[4-[4-[2-[3-[(Dimethylamino)methyl]phenyl]-1H-pyrrolo[2,
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsGSK-1070916 is a potent and selective inhibitor of Aurora B and Aurora C kinases.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionSerine/threonine-protein kinase Aurora-C inhibitor
Product Description

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.

Product Properties

ALogP3.9

Associated Targets

CMTR2 Tbio Cap-specific mRNA (nucleoside-2'-O-)-methyltransferase 2 0 Activities

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

CYP1A2 Tchem Cytochrome P450 1A2 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)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

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

EPHB6 Tchem Ephrin type-B receptor 6 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)

DNAJA1 Tchem DnaJ homolog subfamily A member 1 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)

CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

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

CDKL5 Tchem Cyclin-dependent kinase-like 5 0 Activities

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

CDK17 Tchem Cyclin-dependent kinase 17 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)

FLT4 Tclin Vascular endothelial growth factor receptor 3 0 Activities

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

YES1 Tclin Tyrosine-protein kinase Yes 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 0 Activities

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

FGFR3 Tclin Fibroblast growth factor receptor 3 0 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)

SIK2 Tchem Serine/threonine-protein kinase SIK2 0 Activities

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

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 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)

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

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

BMPR1B Tchem Bone morphogenetic protein receptor type-1B 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 6 Activities

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

AURKB Tchem Aurora kinase B 5 Activities

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

AURKC Tchem Aurora kinase C 5 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)

AAK1 Tchem AP2-associated protein kinase 1 0 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)

ACAD10 Tchem Acyl-CoA dehydrogenase family member 10 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)

ACVRL1 Tchem Serine/threonine-protein kinase receptor R3 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)

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)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

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

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

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

GSK3B Tclin Glycogen synthase kinase-3 beta 0 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)

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

Pubchem Sid488201390
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488201390
IUPAC Name 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea
INCHI InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
InChi Key QTBWCSQGBMPECM-UHFFFAOYSA-N
Canonical SMILES CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC=CC(=C5)CN(C)C
Isomeric SMILES CCN1C=C(C(=N1)C2=CC=C(C=C2)NC(=O)N(C)C)C3=C4C=C(NC4=NC=C3)C5=CC=CC(=C5)CN(C)C
PubChem CID 46885626
Molecular Weight 507.63

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
C23231437Certificate of AnalysisDec 30, 2022 G127938
C23231438Certificate of AnalysisDec 30, 2022 G127938
C23231439Certificate of AnalysisDec 30, 2022 G127938
C23231440Certificate of AnalysisDec 30, 2022 G127938
C23231441Certificate of AnalysisDec 30, 2022 G127938
C23231442Certificate of AnalysisDec 30, 2022 G127938
C23231443Certificate of AnalysisDec 30, 2022 G127938
C23231444Certificate of AnalysisDec 30, 2022 G127938
C23231448Certificate of AnalysisDec 30, 2022 G127938
C23231449Certificate of AnalysisDec 30, 2022 G127938

Chemical and Physical Properties

SolubilityDMSO 102 mg/mL Water <1 mg/mL Ethanol 102 mg/mL

Related Documents

References

1. Girdler F, Gascoigne KE, Eyers PA, Hartmuth S, Crafter C, Foote KM, Keen NJ, Taylor SS.  (2006)  Validating Aurora B as an anti-cancer drug target..  J Cell Sci,  119  (Pt 17): (3664-75).  [PMID:16912073]
2. Andrews PD, Knatko E, Moore WJ, Swedlow JR.  (2003)  Mitotic mechanics: the auroras come into view..  Curr Opin Cell Biol,  15  (6): (672-83).  [PMID:14644191]
3. Keen N, Taylor S.  (2004)  Aurora-kinase inhibitors as anticancer agents..  Nat Rev Cancer,  (12): (927-36).  [PMID:15573114]
4. Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA et al..  (2010)  Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase..  J Med Chem,  53  (10): (3973-4001).  [PMID:20420387]

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