TL-32711 Inhibitor CAS No. 1260251-31-7

Cat. No.	Name	Size	Price	Add Cart
KI3147	TL-32711	5 mg	$592
KI3147	TL-32711	50 mg	$2720

Chemical Characteristic

Product Name	TL-32711
Synonyms	Birinapant
CAS No.	1260251-31-7
Molecular Weight	806.91
Formula	C₄₂H₅₆F₂N₈O₆
Chemical Name	(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)
Smiles	C(=O)([C@H](C)NC)NC(C(=O)N1[C@@H](C[C@@H](C1)O)Cc1c([nH]c2c1ccc(c2)F)c1[nH]c2c(c1CC1N(C[C@H](C1)O)C(=O)[C@H](CC)NC(=O)[C@H](C)NC)ccc(c2)F)CC
Chemical Structure

Biological activities

TL32711 is a mimic of Smac, natural inhibitor of IAPs. TL32711 binds to the IAPs in tumor cells and inhibits their function leading to the activation of apoptotic cell death and shutdown of the survival pathway.^[1] TL32711 induces cell death in TRAIL-insensitive SUM190 cells with an IC50 of ~300 nM. In vitro, TL32711 inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively.^[2]

Protocols

In vivo, TL32711 is dissolved in 12.5% Captisol (Ligand Pharmaceuticals) in distilled water.^[3]

References

[1]Fetterly G J, Liu B, Senzer N N, et al. Clinical pharmacokinetics of the smac-mimetic birinapant (TL32711) as a single agent and in combination with multiple chemotherapy regimens[J]. Breast. 2012, 4 (1): 1. [2]Allensworth JL, et al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-?-independent mechanism. Breast Cancer Res Treat. 2013, 137 (2): 359-371. [3]Krepler C, et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013, 19 (7):1784-94.

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