cb-5083

Description: CB-5083 is a novel, potent, selective, first in class and orally bioavailable p97 AAA ATPase inhibitor with potential anticancer activity. It inhibits p97 AAA ATPase with an IC50 of 11 nM. CB-5083 disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer.

References: J Med Chem. 2015 Dec 24; 58(24):9480-97.

Synonym: CB5083; CB-5083; CB 5083.

Chemical Name: 1-(4-(benzylamino)-7, 8-dihydro-5H-pyrano[4, 3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide

InChi Key: RDALZZCKQFLGJP-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9, 12H, 10-11, 13-14H2, 1H3, (H2, 25, 30)(H, 26, 27, 28)

SMILES Code: O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.