Birinapant

Catalog No.S7015 Synonyms: TL32711

Birinapant Chemical Structure

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.

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4 Customer Reviews

  • 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.

  • (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.

    Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.

    Cell Death Dis 2013 4, e951. Birinapant purchased from Selleck.

Purity & Quality Control

Choose Selective IAP Inhibitors

Biological Activity

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.
Targets
cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
<1 nM(Kd) 45 nM(Kd)
In vitro

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. [1] 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.[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3frfFUxNzJyMD:1NFAhdk1? Ml7RNE06PiCq M2DOb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ MkHxNlYzPTJ7Nkm=
Molm13  NFf4S5hHfW6ldHnvckBCe3OjeR?= MnPkNk8zOC9{MECgcm0> MoP1NlQhcA>? Mnjm[IVkemWjc3XzJINKSVBzIHHu[EwhfG9iYTDteYNpKGync4PldkBmgHSnboSsJINKSVB{LDDhcoQhYEmDUDD1coRmeiC4YYLpc5V{KGOxbnTpeIlwdnN? MnPVNlQ2OjZ5OEe=
WTH202 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS3NkBp MUXJR|UxRTFwODDuUUwh[2:vYnnu[YQhf2m2aDCxcocwdWxiVF7GMe6y MVSyN|QxOzZ|NB?=
WM793B NVm3WHM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXS3NkBp NGXleVdKSzVyPUKuOUBvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z NHrt[JQzOzRyM{[zOC=>
WM9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG3NkBp M3qwN2lEPTB;Mj60JI5O MmrJNlM1ODN4M{S=
WM9 NVjjVm41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzDems4OiCq M1LPRWlEPTB;Mj63JI5ONCClb33ibY5m\CC5aYToJFFv\y:vbDDUUmYu|rF? MUiyN|QxOzZ|NB?=
WM1366 NITI[ppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDVS2U4OiCq M3KzTmlEPTB;Nz65JI5ONCClb33ibY5m\CC5aYToJFFv\y:vbDDUUmYu|rF? NHXXbmkzOzRyM{[zOC=>
WM164 NVnIVVNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TOUFczKGh? MUDJR|UxRTlibl2sJINwdWKrbnXkJJdqfGhiMX7nM41tKFSQRj5OtS=> MXuyN|QxOzZ|NB?=
451Lu MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DwNlczKGh? MULJR|UxRTF2LkKgcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? MYiyN|QxOzZ|NB?=
WM1341D MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYO3NkBp NH3LVmVKSzVyPUW3MlYhdk1uIHPvcYJqdmWmIIfpeIghOW6pL33sJHRPTi4QsR?= NIDJSHozOzRyM{[zOC=>
WM3130 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKyO|IhcA>? MUPJR|UxRTZ2LkOgcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? MUiyN|QxOzZ|NB?=
WM1985 NGnhXHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrZO5E4OiCq MX;JR|UxRTl5IH7NMEBkd22kaX7l[EB4cXSqIEHu[{9udCCWTl[t{tE> MnzDNlM1ODN4M{S=
WM3854 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qwVVczKGh? NUXSUmp2UUN3ME2yNlYhdk1uIHPvcYJqdmWmIIfpeIghOW6pL33sJHRPTi4QsR?= NWHRSpVXOjN2MEO2N|Q>

... Click to View More Cell Line Experimental Data

In vivo Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. [2]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[2]
+ Expand
  • Cell lines: Human melanoma cell lines WM9
  • Concentrations: 1 nM-1 μM
  • Incubation Time: 3 days
  • Method: Cells are allowed to attach for 24 hours and subsequently incubated with Birinapant and/or TNF-α for 24 or 72 hours. Then MTS assay is conducted
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Human melanoma xenografts 451Lu
  • Formulation: 12.5% Captisol in distilled water
  • Dosages: 30 mg/kg
  • Administration: 3 times per week intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (123.92 mM)
Ethanol 55 mg/mL (68.15 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
15% Captisol
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 806.94
Formula

C42H56F2N8O6

CAS No. 1260251-31-7
Storage powder
in solvent
Synonyms TL32711

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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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID