AZ0108

    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.

Chemical Structure

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AZ0108
CAS# 1825345-52-5
Instruction

Theoretical Analysis

MedKoo Cat#: 407208
Name: AZ0108
CAS#: 1825345-52-5
Chemical Formula: C24H20F4N6O2
Exact Mass: 500.16
Molecular Weight: 500.458
Elemental Analysis: C, 57.60; H, 4.03; F, 15.18; N, 16.79; O, 6.39

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 500.46 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.