AZD2461 - ≥98%, high purity , CAS No.1174043-16-3

Item Number
A127274
Grouped product items
SKUSizeAvailabilityPrice Qty
A127274-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$124.90
A127274-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$562.90
A127274-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$567.90

Potent PARP inhibitor

Basic Description

SynonymsNCGC00381558-06 | 4-{[4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl}phthalazin-1(2H)-one | BDBM50288530 | s7029 | 1174043-16-3 | HYNBNUYQTQIHJK-UHFFFAOYSA-N | 3K288XF5XJ | AC-36007 | 4-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalaz
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent PARP inhibitor (IC50values are 2, 5 and 200 nM for PARP2, PARP1 and PARP3, respectively). Exhibits anticancer effects inBRCA1mutant, but not wild-type breast cancer cell linesin vitro. Inhibits growth of olaparib-resistant mammary tumors in a mouse
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Note卖完停产,不再备货
Product Description

AZD2461 is a novel PARP inhibitor, which has the potential to avoid the olaparib resistence mediated by Pgp.

Associated Targets(Human)

PRAP1 Tchem Proline-rich acidic protein 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PARP1 Tclin Poly [ADP-ribose] polymerase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PARP1 Tclin Poly [ADP-ribose] polymerase-1 (6206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF-10A (2462 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF7 (126967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-468 (9477 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MEF (1005 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 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-[[4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one
INCHI InChI=1S/C22H22FN3O3/c1-29-15-8-10-26(11-9-15)22(28)18-12-14(6-7-19(18)23)13-20-16-4-2-3-5-17(16)21(27)25-24-20/h2-7,12,15H,8-11,13H2,1H3,(H,25,27)
InChi Key HYNBNUYQTQIHJK-UHFFFAOYSA-N
Canonical SMILES COC1CCN(CC1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=CC=CC=C43)F
Isomeric SMILES COC1CCN(CC1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=CC=CC=C43)F
PubChem CID 44199317
Molecular Weight 395.43

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

4 results found

Lot NumberCertificate TypeDateItem
L2322065Certificate of AnalysisJan 03, 2024 A127274
E1609027Certificate of AnalysisOct 16, 2023 A127274
A1822015Certificate of AnalysisJun 08, 2023 A127274
A1822016Certificate of AnalysisJun 08, 2023 A127274

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 39.54, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 39.54, Max Conc. mM: 100

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS07
Signal Warning
Hazard Statements

H373:Causes damage to organs through prolonged or repeated exposure

H302:Harmful if swallowed

Precautionary Statements

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

P319:Get medical help if you feel unwell.

Related Documents

References

1. Graziani G, Szabó C.  (2005)  Clinical perspectives of PARP inhibitors..  Pharmacol Res,  52  (1): (109-18).  [PMID:15911339] [10.1021/op500134e]
2. Jaspers JE, Kersbergen A, Boon U, Sol W, van Deemter L, Zander SA, Drost R, Wientjens E, Ji J, Aly A et al..  (2013)  Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors..  Cancer Discov,  (1): (68-81).  [PMID:23103855] [10.1021/op500134e]

Solution Calculators