Ro3280 - ≥99%, high purity , CAS No.1062243-51-9, Inhibitor of FER tyrosine kinase;Inhibitor of polo like kinase 1;Inhibitor of TTK protein kinase

Item Number
R127227
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R127227-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$121.90
R127227-10mg
10mg
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$194.90
R127227-25mg
25mg
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$389.90
R127227-50mg
50mg
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$613.90
R127227-100mg
100mg
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$999.90

Potent and selective PLK1 inhibitor

Basic Description

SynonymsBCP05205 | HMS3653O21 | PharmaGSID_48511 | 1-ethyl-7-methyl-4-oxo-1,8-naphthyridine-3-carboxylic acid | 4-((9-Cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzam
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsPotent and selective PLK inhibitor (IC50= 3 nM). Exhibits selectivity for PLK1 over a panel of other kinases. Inhibits growth of a range of tumor cells linesin vitroand induces apoptosis in leukemia cells. Exhibits antitumor activity in mouse colorectal
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of FER tyrosine kinase;Inhibitor of polo like kinase 1;Inhibitor of TTK protein kinase

Associated Targets(Human)

FER Tclin Tyrosine-protein kinase Fer (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TTK Tchem Dual specificity protein kinase TTK (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PLK1 Tchem Serine/threonine-protein kinase PLK1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HT-29 (80576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRDT Tchem Bromodomain testis-specific protein (576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MM1.S (1111 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
INCHI InChI=1S/C27H35F2N7O3/c1-34-12-10-18(11-13-34)31-24(37)17-8-9-20(22(14-17)39-3)32-26-30-15-21-23(33-26)36(19-6-4-5-7-19)16-27(28,29)25(38)35(21)2/h8-9,14-15,18-19H,4-7,10-13,16H2,1-3H3,(H,31,37)(H,30,32,33)
InChi Key DJNZZLZKAXGMMC-UHFFFAOYSA-N
Canonical SMILES CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC
Isomeric SMILES CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC
PubChem CID 25015677
Molecular Weight 543.61

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
E2431401Certificate of AnalysisFeb 26, 2024 R127227
E2431415Certificate of AnalysisFeb 26, 2024 R127227
E2431416Certificate of AnalysisFeb 26, 2024 R127227
E2431417Certificate of AnalysisFeb 26, 2024 R127227
E2431418Certificate of AnalysisFeb 26, 2024 R127227
E2431419Certificate of AnalysisFeb 26, 2024 R127227
E2431420Certificate of AnalysisFeb 26, 2024 R127227
E2431421Certificate of AnalysisFeb 26, 2024 R127227
E2431422Certificate of AnalysisFeb 26, 2024 R127227
E2431423Certificate of AnalysisFeb 26, 2024 R127227

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 27.18, Max Conc. mM: 50; Solvent:ethanol, Max Conc. mg/mL: 27.18, Max Conc. mM: 50

Related Documents

References

1. Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S et al..  (2012)  Identification of novel, potent and selective inhibitors of Polo-like kinase 1..  Bioorg Med Chem Lett,  22  (2): (1247-50).  [PMID:22172702] [10.1021/op500134e]

Solution Calculators