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PHASE 2 -TetraLogic’s BIRINAPANT for treatment of acute myeloid leukemia, pancreatic cancer, or ovarian cancer

November 29, 2013 9:45 am


DR ANTHONY MELVIN CRASTO Ph.D's avatarNew Drug Approvals

ChemSpider 2D Image | Birinapant | C42H56F2N8O6

BIRINAPANT, Apoptosis inhibitor

(2S,2’S)-N,N’-((2S,2’S)-((3S,3’S,5R,5’R)-5,5′-((6,6′-difluoro-1H,1’H-[2,2′-biindole]-3,3′-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide)

1260251-31-7 cas no

Birinapant is an antagonist of XIAP and cIAP1 with Kd value of 45 nM and <1 nM, respectively.

US20110003877,WO 2013049350 A1

Molecular Weight:806.94
Birinapant Formula:C42H56F2N8O6

Birinapant, also known as TL32711,  is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity. As a SMAC mimetic and IAP antagonist, TL32711 binds to and inhibits the activity of IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9…

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Posted by DR ANTHONY MELVIN CRASTO Ph.D

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One Response to “PHASE 2 -TetraLogic’s BIRINAPANT for treatment of acute myeloid leukemia, pancreatic cancer, or ovarian cancer”

  1. Reblogged this on MED.CHEM in BURMA.

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    By sonsondaimari on December 1, 2013 at 1:06 am

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