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.

  • 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.

    (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.

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.
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 MlHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXpOVAwOjByL{WwNEBvVQ>? MWCwMVk3KGh? M{naSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NIP5c|YzPjJ3Mkm2PS=>
Molm13  NIHGfVdHfW6ldHnvckBCe3OjeR?= M4LTO|IwOjBxMkCwJI5O NX;tdHNUOjRiaB?= NInwcmhl\WO{ZXHz[ZMh[0mDUEGgZY5lNCC2bzDhJI12[2hibHXzd4VzKGW6dHXueEwh[0mDUEKsJIFv\CC[SVHQJJVv\GW{II\hdolwfXNiY3;u[Il1cW:wcx?= MWCyOFUzPjd6Nx?=
WTH202 NETVNVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rHXFczKGh? MXvJR|UxRTFwODDuUUwh[2:vYnnu[YQhf2m2aDCxcocwdWxiVF7GMe6y M{jGOVI{PDB|NkO0
WM793B NEXo[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf1UHc4PzJiaB?= M3\Ye2lEPTB;Mj61JI5ONCClb33ibY5m\CC5aYToJFFv\y:vbDDUUmYu|rF? MXeyN|QxOzZ|NB?=
WM9 NXLxWHNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnLRVkzPzJiaB?= MnS1TWM2OD1{LkSgcm0> NHTiXIkzOzRyM{[zOC=>
WM9 Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;sO|IhcA>? NIPz[mVKSzVyPUKuO{BvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z MWqyN|QxOzZ|NB?=
WM1366 NX31WlJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnMUXZEPzJiaB?= NV;2VJF1UUN3ME23Mlkhdk1uIHPvcYJqdmWmIIfpeIghOW6pL33sJHRPTi4QsR?= M1jnbVI{PDB|NkO0
WM164 MnfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLQR4s4OiCq M4fxS2lEPTB;OTDuUUwh[2:vYnnu[YQhf2m2aDCxcocwdWxiVF7GMe6y M37X[lI{PDB|NkO0
451Lu NUnjOoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3NkBp MXHJR|UxRTF2LkKgcm0tKGOxbXLpcoVlKHerdHigNY5oN22uIGTOSk3PuQ>? NXrDVHZTOjN2MEO2N|Q>
WM1341D NX2ySY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NkBp M2[5cmlEPTB;NUeuOkBvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z M1fObFI{PDB|NkO0
WM3130 NX3mWoRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi3NkBp M3;rbmlEPTB;NkSuN{BvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z MUeyN|QxOzZ|NB?=
WM1985 M33LPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37GeFczKGh? NUD0[3FrUUN3ME25O{BvVSxiY3;tZolv\WRid3n0bEAydmdxbXygWG5HNc7z MlrZNlM1ODN4M{S=
WM3854 NEHsSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjVfVhrPzJiaB?= MUHJR|UxRTJ{NjDuUUwh[2:vYnnu[YQhf2m2aDCxcocwdWxiVF7GMe6y NWXDToFKOjN2MEO2N|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]


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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.
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


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
NCT02756130 Withdrawn High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) August 1 2018 Phase 1|Phase 2
NCT02587962 Recruiting Solid Tumors Medivir|Merck Sharp & Dohme Corp. August 4 2017 Phase 1|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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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID