1403898-55-4

1403898-55-4 structure

Name: AT-IAP
Chemical Name: 1-[6-(4-Fluorobenzyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-{[(3R)-3-methyl-4-morpholinyl]methyl}-1-piperazinyl]ethanone
CAS Number: 1403898-55-4
Molecular Formula: C₂₉H₄₀FN₅O₂
Molecular Weight: 509.659
Catalog: Signaling Pathways Apoptosis IAP
Create Date: 2020-01-11 17:53:50
Modify Date: 2024-04-04 18:05:56
A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts.

Name	1-[6-(4-Fluorobenzyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-{[(3R)-3-methyl-4-morpholinyl]methyl}-1-piperazinyl]ethanone
Synonyms	Ethanone, 1-[6-[(4-fluorophenyl)methyl]-2,3-dihydro-3,3-dimethyl-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methyl-4-morpholinyl]methyl]-1-piperazinyl]- 1-[6-(4-Fluorobenzyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-{[(3R)-3-methyl-4-morpholinyl]methyl}-1-piperazinyl]ethanone

Description	A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts.
References	References 1. Tamanini E, et al. J Med Chem. 2017 Jun 8;60(11):4611-4625. 2. Armstrong CW, et al. Oncotarget. 2016 Feb 16;7(7):7885-98. View Related Products by Target IAP