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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | NCGC00381558-06 | 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 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent 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 Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
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. |
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IUPAC Name | 4-[[4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one |
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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 |
PubChem CID | 44199317 |
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CAS Registry No. | 1174043-16-3 |
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Solubility | Solvent:DMSO, Max Conc. mg/mL: 39.54, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 39.54, Max Conc. mM: 100 |
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Pictogram(s) | GHS08, GHS07 |
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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. |
1. Graziani G, Szabó C. (2005) Clinical perspectives of PARP inhibitors.. Pharmacol Res, 52 (1): (109-18). [PMID:15911339] |
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, 3 (1): (68-81). [PMID:23103855] |