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 5 Publications
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Western blot from tumours harvested at day 5 after treatment showing an increase in PARP cleavage in the irinotecan-treated group.
British Journal of Cancer, 2015, 112: 1471–1479. Birinapant purchased from Selleck.
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.
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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||15% Captisol||5 mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02587962||Not yet recruiting||Solid Tumors||TetraLogic Pharmaceuticals|Merck Sharp & Dohme Corp.||February 2017||Phase 1|Phase 2|
|NCT02756130||Not yet recruiting||Advanced Newly Diagnosed or Recurrent High Grade Serous Carcinomas (HGSC)||Jonsson Comprehensive Cancer Center|TetraLogic Pharmaceuticals||January 2017||Phase 2|
|NCT02288208||Terminated||Hepatitis B||TetraLogic Pharmaceuticals||November 2014||Phase 1|
|NCT02147873||Terminated||Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML)||TetraLogic Pharmaceuticals||June 2014||Phase 2|
|NCT01940172||Completed||Relapsed Epithelial Ovarian Cancer|Relapsed Primary Peritoneal Cancer|Relapsed Fallopian Tube Cancer||TetraLogic Pharmaceuticals||November 2013||Phase 1|
|NCT01828346||Completed||Myelodysplastic Syndrome||TetraLogic Pharmaceuticals||June 2013||Phase 1|Phase 2|
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