Name: Birinapant (TL32711)
Brand: Selleck Chemicals
SKU: S7015
Availability: InStock
Rating: 5 (84 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Products Often Used Together with Birinapant (TL32711)

Zosuquidar 3HCl

In combination with Zosuquidar, it induces death of HBV-positive liver cells and improves HBV surface antigen (HBsAg) control kinetics in an immunocompetent mouse model of HBV infection.

Related Targets	Bcl-2 Caspase K-Ras PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha
Other IAP Inhibitors	SM-164 BV6 LCL161 Xevinapant (AT406) GDC-0152 AZD5582 Tolinapant (ASTX660)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PANC-1	Growth Inhibition Assay	50/200/500 nM	0-96 h	inhibits cell growth in both time and dose dependent manner	26252969
Molm13	Function Assay	2/20/200 nM	24 h	decreases cIAP1 and, to a much lesser extent, cIAP2, and XIAP under various conditions	24526787
WTH202	Growth Inhibition Assay		72 h	IC50=1.8 nM, combined with 1ng/ml TNF-α	23403634
WM793B	Growth Inhibition Assay		72 h	IC50=2.5 nM, combined with 1ng/ml TNF-α	23403634
WM9	Growth Inhibition Assay		72 h	IC50=2.4 nM	23403634
WM9	Growth Inhibition Assay		72 h	IC50=2.7 nM, combined with 1ng/ml TNF-α	23403634
WM1366	Growth Inhibition Assay		72 h	IC50=7.9 nM, combined with 1ng/ml TNF-α	23403634
WM164	Growth Inhibition Assay		72 h	IC50=9 nM, combined with 1ng/ml TNF-α	23403634
451Lu	Growth Inhibition Assay		72 h	IC50=14.2 nM, combined with 1ng/ml TNF-α	23403634
WM1341D	Growth Inhibition Assay		72 h	IC50=57.6 nM, combined with 1ng/ml TNF-α	23403634
WM3130	Growth Inhibition Assay		72 h	IC50=64.3 nM, combined with 1ng/ml TNF-α	23403634
WM1985	Growth Inhibition Assay		72 h	IC50=97 nM, combined with 1ng/ml TNF-α	23403634
WM3854	Growth Inhibition Assay		72 h	IC50=226 nM, combined with 1ng/ml TNF-α	23403634
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against cIAP/XIAP-dependent human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.01 μM.	25584393
A875	Cytotoxicity assay		72 hrs	Cytotoxicity against XIAP-dependent human A875 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.04 μM.	25584393
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (123.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (7.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (0.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	806.94	Formula	C₄₂H₅₆F₂N₈O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1260251-31-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TL32711			Smiles	CCC(C(=O)N1CC(CC1CC2=C(NC3=C2C=CC(=C3)F)C4=C(C5=C(N4)C=C(C=C5)F)CC6CC(CN6C(=O)C(CC)NC(=O)C(C)NC)O)O)NC(=O)C(C)NC

Mechanism of Action

Targets/IC₅₀/Ki	cIAP1 (Cell-free assay) <1 nM(Kd) XIAP (Cell-free assay) 45 nM(Kd)
In vitro	Birinapant binds with XIAP and cIAP1 with K_d of 45 and <1 nM, respectively. This compound 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. It causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. This chemical in combination with TNF-α exhibits a strong antimelanoma effect in vitro. It 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. This compound singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. It significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.
Kinase Assay	Fluorescence polarization assay
Kinase Assay	The binding affinities of compounds to XIAP and cIAP1 are determined using a fluorogenic substrate and are reported as K_d values. Initially, the dissociation constant (K_d) 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 vivo	Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23225169/ [2] https://pubmed.ncbi.nlm.nih.gov/23403634/

Applications

Methods	Biomarkers	PMID
Western blot	cIAP1 / cIAP2 / XIAP NF-κB(p65) / IκBa / Bcl-xl / NF-κB(p100) / p52 BIRC2 / ARC	24526787
Immunofluorescence	Caspase 3/7	28665401
Growth inhibition assay	Cell viability	28460471

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01681368	Terminated	Epithelial Ovarian Cancer\|Peritoneal Neoplasms\|Fallopian Tube Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	August 15 2012	Phase 2
NCT01486784	Terminated	Acute Myelogenous Leukemia	Abramson Cancer Center at Penn Medicine	November 2011	Phase 1\|Phase 2

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Handling Instructions

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Birinapant (TL32711) IAP antagonist

Chemical Structure

Molecular Weight: 806.94