WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407207
CAS#: 1825345-33-2
Description: AZ9482 is a potent and selective PARP inhibitor featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent centrosome declustering activity in HeLa cells (EC50 < 18 nM). Encouragingly, AZ9482 also showed a 3 nM GI50 in the DLBCL cell line OCI-LY-19 in a 3-day AlamarBlue assay. Consistent with published siRNA knockdown experiments, AZ9482 was a 9 nM enzyme inhibitor of tankyrase 1 (TNKS1).
MedKoo Cat#: 407207
Name: AZ9482
CAS#: 1825345-33-2
Chemical Formula: C26H22N6O2
Exact Mass: 450.18042
Molecular Weight: 450.502
Elemental Analysis: C, 69.32; H, 4.92; N, 18.66; O, 7.10
Synonym: AZ9482; AZ-9482; AZ 9482.
IUPAC/Chemical Name: 2-(4-(3-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)nicotinonitrile
InChi Key: ZDDPBFWHZOJFHF-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H22N6O2/c27-17-20-7-4-10-28-24(20)31-11-13-32(14-12-31)26(34)19-6-3-5-18(15-19)16-23-21-8-1-2-9-22(21)25(33)30-29-23/h1-10,15H,11-14,16H2,(H,30,33)
SMILES Code: O=C1NN=C(CC2=CC=CC(C(N3CCN(C4=NC=CC=C4C#N)CC3)=O)=C2)C5=CC=CC=C51
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 450.502 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Jeffrey W. Johannes, Lynsie Almeida, Kevin Daly, Andrew D. Ferguson, Shaun E. Grosskurth, Huiping Guan, Tina Howard, Stephanos Ioannidis, Steven Kazmirski, Michelle L. Lamb, Nicholas A. Larsen, Paul D. Lyne, Keith Mikule, Claude Ogoe, Bo Peng, Philip Petteruti, Jon A. Read, Nancy Su, Mark Sylvester, Scott Throner, Wenxian Wang, et al. Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering
In Press, Corrected Proof, Available online 27 October 2015. Bioorg. Med. Chem . Lett. 2015.
