WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407913
Description: AZ32 is an orally bioavailable and blood-brain-barrier penetrating ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice. AZ32 was highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is the first ATMi with oral bioavailability shown to radiosensitize glioma and improve survival in orthotopic mouse models.
MedKoo Cat#: 407913
Chemical Formula: C20H16N4O
Exact Mass: 328.1324
Molecular Weight: 328.375
Elemental Analysis: C, 73.15; H, 4.91; N, 17.06; O, 4.87
Synonym: AZ32; AZ-32; AZ 32.
IUPAC/Chemical Name: N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
InChi Key: LCRTUEXVVKVKBD-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H16N4O/c1-21-20(25)16-9-7-15(8-10-16)18-11-23-19-12-22-17(13-24(18)19)14-5-3-2-4-6-14/h2-13H,1H3,(H,21,25)
SMILES Code: O=C(NC)C(C=C1)=CC=C1C2=CN=C3C=NC(C4=CC=CC=C4)=CN32
Inhibition of ataxia-telangiectasia mutated (ATM) during radiotherapy of glioblastoma multiforme (GBM) may improve tumor control by short-circuiting the response to radiation-induced DNA damage. A major impediment for clinical implementation is that current inhibitors have limited CNS bioavailability, thus, the goal was to identify ATM inhibitors (ATMi) with improved CNS penetration.
1: Karlin J, Allen J, Ahmad SF, Hughes G, Sheridan V, Odedra R, Farrington P, Cadogan EB, Riches LC, Garcia-Trinidad A, Thomason AG, Patel B, Vincent J, Lau A, Pike KG, Hunt TA, Sule A, Valerie NCK, Biddlestone-Thorpe L, Kahn J, Beckta JM, Mukhopadhyay N, Barlaam B, Degorce SL, Kettle J, Colclough N, Wilson J, Smith A, Barrett IP, Zheng L, Zhang T, Wang Y, Chen K, Pass M, Durant ST, Valerie K. Orally bioavailable and blood-brain-barrier penetrating ATM inhibitor (AZ32) radiosensitizes intracranial gliomas in mice. Mol Cancer Ther. 2018 May 16. pii: molcanther.0975.2017. doi: 10.1158/1535-7163.MCT-17-0975. [Epub ahead of print] PubMed PMID: 29769307.