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 |
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 |