Dasminapant
CAS 1570231-89-8
| Molecular Weight | 1157.40 |
|---|---|
| Formula | C60H72N10O10S2 |
| APG-1387, SM-1387, E53VN70K2X, INN 12430, APG-1387 UNII-E53VN70K2X APG-1387 (SMAC MIMETIC) SMAC-mimetic APG-1387 IAP Inhibitor APG-1387 |
| (5S,5’S,8S,8’S,10aR,10’aR)-3,3′-[1,3-phenylenebis(sulfonyl)]bis{N-(diphenylmethyl)-5-[(2S)-2-(methylamino)propanamido]-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide} |
(5S,8S,10aR)-3-[3-[[(5S,8S,10aR)-8-(benzhydrylcarbamoyl)-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocin-3-yl]sulfonyl]phenyl]sulfonyl-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
Dasminapant (APG-1387), a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). Dasminapant induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. Dasminapant can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
Dasminapant, also known as APG-1387 and SM-1387, is a IAP inhibitor. APG-1387 promotes the rapid degradation of cIAP1/2 and XIAP, and it exerts an antitumor effect on nasopharyngeal carcinoma cancer stem cells. Further studies show that APG-1387 enhances the chemosensitivity and promotes apoptosis in combination with CDDP and 5-FU of NPC in vitro and vivo.
PATENTS
WO2022012671
PATENT
WO2014031487 …
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014031487&_cid=P11-MAJOJ5-33000-1
PATENT
US20140057924
SCHEME
///////////////Dasminapant, APG-1387, SM-1387, E53VN70K2X, INN 12430, APG 1387, UNII-E53VN70K2X, APG-1387 (SMAC MIMETIC), SMAC-mimetic APG-1387, IAP Inhibitor APG-1387, SM 1387