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Molecular Weight: 421.36
Description
An inhibitor of PARP1 with Ki of 1.4 nM in a cell-free assay and also showing binding affinity to eight other PARP domains.
Chemical structure:
Molecular formula: C19H18FN3O.H3PO4
CAS Number: 459868-92-9
Purity: ≥98% by HPLC
Storage: Store powder at 4°C protected from light. Stock solutions at -20°C are stable for 6 months
Solubility: Soluble in DMSO
References:
Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) restrict oral availability and brain accumulation of the PARP inhibitor rucaparib (AG-014699). Durmus S, Sparidans RW, van Esch A, Wagenaar E, Beijnen JH, Schinkel AH. Pharm Res. 2015 Jan;32(1):37-46. doi: 10.1007/s11095-014-1442-z. Epub 2014 Jun 25. PMID: 24962512
NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Hunter JE, Willmore E, Irving JA, Hostomsky Z, Veuger SJ, Durkacz BW. Oncogene. 2012 Jan 12;31(2):251-64. doi: 10.1038/onc.2011.229. Epub 2011 Jun 27.
PMID: 21706052
Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Daniel RA, Rozanska AL, Mulligan EA, Drew Y, Thomas HD, Castelbuono DJ, Hostomsky Z, Plummer ER, Tweddle DA, Boddy AV, Clifford SC, Curtin NJ. Br J Cancer. 2010 Nov 9;103(10):1588-96. doi: 10.1038/sj.bjc.6605946. Epub 2010 Oct 26. PMID: 20978505
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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