WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407208
CAS#: 1825345-52-5
Description: AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. Consistent with this lack of potencytowards tankyrase, AZ0108 is not active in a DLD-1 Wnt luciferase reporter assay.
MedKoo Cat#: 407208
Name: AZ0108
CAS#: 1825345-52-5
Chemical Formula: C24H20F4N6O2
Exact Mass: 500.1584
Molecular Weight: 500.4576
Elemental Analysis: C, 57.60; H, 4.03; F, 15.18; N, 16.79; O, 6.39
Synonym: AZ0108; AZ-0108; AZ 0108.
IUPAC/Chemical Name: (S)-4-((3-(3-(1,1-difluoroethyl)-6-methyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)phenyl)difluoromethyl)phthalazin-1(2H)-one
InChi Key: NWGMIELHSCQGOG-ZDUSSCGKSA-N
InChi Code: InChI=1S/C24H20F4N6O2/c1-13-11-34-18(29-32-22(34)23(2,25)26)12-33(13)21(36)14-6-5-7-15(10-14)24(27,28)19-16-8-3-4-9-17(16)20(35)31-30-19/h3-10,13H,11-12H2,1-2H3,(H,31,35)/t13-/m0/s1
SMILES Code: FC(F)(C1=CC=CC(C(N2[C@H](CN3C(C2)=NN=C3C(F)(C)F)C)=O)=C1)C4=NNC(C5=CC=CC=C54)=O
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 500.4576 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 |
1: Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T,
Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B,
Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q,
Yu Y, Zheng X, Scott DA. Discovery of AZ0108, an orally bioavailable
phthalazinone PARP inhibitor that blocks centrosome clustering. Bioorg Med Chem
Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct
27. PubMed PMID: 26546219.
