AT-IAP

Names

[ Name ]:
AT-IAP

[Synonym ]:
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

Biological Activity

[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

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
678.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₉H₄₀FN₅O₂

[ Molecular Weight ]:
509.659

[ Flash Point ]:
364.0±31.5 °C

[ Exact Mass ]:
509.316589

[ LogP ]:
4.23

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.549

Related Compounds

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