Catalog No.S7015 Synonyms: TL32711
Molecular Weight(MW): 806.94
Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Phase 2.
Cited by 15 Publications
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Cell survival of macrophages was measured by MTT assay after(a) 24 h and (b) 2 or 4 h posttreatment of cells with SMAC mimetic (BP, 10 μM) with or without zVAD-fmk (50 μM) or Nec-1 (10 μM). Graphs show the percentage of surviving cells relative to the corresponding vehicle control. These graphs are representative of three biological replicates each carried out in triplicate.
Cell Death Differ, 2016, 23(10):1628-37.. Birinapant purchased from Selleck.
(a) Apoptosis assessed morphologically after DAPI staining (top panels) and by caspase 3/7 activation (bottom panels) in human cholangiocyte cell lines H69 and NHC, and the human breast cancer cell line MDA-MB-231, incubated for 24 h with or without (cnt) the SMAC mimetic TL32711 (1 μM), in the presence or absence of neutralizing antibodies against TNFα (1 μg/ml) or FasL (1 μg/ml), or recombinant TRAIL-R2:Fc (1 μg/ml).
Cell Death Dis, 2017, 8(1):e2535. Birinapant purchased from Selleck.
FTC cell lines were treated with increasing concentrations of rh-TRAIL with and without Smac mimetics Birinapant (A/B). Changes in cell viability are illustrated linearly in percentage control and stratified according to the FP. While FTC cell line TT2609-C02 was susceptible to rh-TRAIL alone (A), cell line FTC133 proved to be resistant to rh-TRAIL induced apoptosis (B). Smac mimetic treatment alone had no impact on cell viability. Annexin-V/PI staining and FACS analyses of FTC cells demonstrate the changes of annexin positive apoptotic cells after incubation with rh-TRAIL alone (-) or in combination (+) with Smac mimetics Birinapant. Changes in protein expression of cIAP1/2 after treatment with the respective Smac mimetic are illustrated using western blot. GAPDH served as loading control. Blots are cropped to increase clarity. Statistical significance was calculated by two-tailed nonparametric Mann-Whitney test. e. survival = expected survival, sp. survival = specific survival, FP = fractional product; *p < 0.05; **p < 0.01.
Endocr Relat Cancer, 2018, 25(3):295-308. Birinapant purchased from Selleck.
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|Description||Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Phase 2.|
Birinapant binds with XIAP and cIAP1 with Kd of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation.  Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. Birinapant in combination with TNF-α(1 ng/mL) 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, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.
|In vivo||Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. |
Fluorescence polarization assay:The binding affinities of compounds to XIAP and cIAP1 are determined using a fluorogenic substrate and are reported as Kd values. Initially, the dissociation constant (Kd) for the fluorescently labeled modified Smac peptide (AbuRPF-K(5-Fam)-NH2; FP pep-tide) is determined using a fixed concentration of peptide (5 nM) and titrating varying concentrations of protein (0.075–5 μM in half log dilutions). The dose–response curves are produced by a nonlinear least squares fit to a single-site binding model using GraphPad Prism, with 5 nM of FP peptide and 50 nM of XIAP used in the assay. Various concentrations of Smac mimetics (100–0.001 μM in half log dilutions) are added to FP peptide:protein binary complex for 15 min at room temperature in 100μL of 0.1 M potassium phosphate buffer, pH 7.5, containing 100 mg/mL bovine c -globulin. Following incubation, the polarization values are measured on a multi-label plate reader using a 485 nm excitation filter and a 520 nm emission filter.
|In vitro||DMSO||100 mg/mL (123.92 mM)|
|Ethanol||55 mg/mL (68.15 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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