Birinapant (TL32711) (Synonyms: TL-32711)

Name: Birinapant (TL32711)
Brand: GlpBio
SKU: GC12426
Availability: InStock
Rating: 5 (30 reviews)

رقم الكتالوجGC12426

مضاد لـ cIAP1 و cIAP2 و XIAP

Products are for research use only. Not for human use. We do not sell to patients.

Birinapant (TL32711) التركيب الكيميائي

Cas No.: 1260251-31-7

الحجم

السعر

المخزون

الكميّة

10mM (in 1mL DMSO)	93٫00	متوفر
5mg	65٫00	متوفر
10mg	104٫00	متوفر
25mg	165٫00	متوفر
50mg	237٫00	متوفر

Tel：(909) 407-4943 Email: sales@glpbio.com

مراجعات العميل

بناء على آراء العملاء.

Sample solution is provided at 25 µL, 10mM.

منتجات GlpBio المذكورة في الأوراق ذات السمعة الطيبة

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

View current batch:

Purity: >99.50%

Protocol

IAP binding affinity of Birinapant (TL32711)[1]:
Preparation Method	A fluorescence polarization assay was used to determine the dissociation constants (K d) of Smac mimetics Birinapant (TL32711) and GT13402 for XIAP and cIAP1 by monitoring the decrease in fluorescence polarization signal due to competitive displacement of an FP peptide from the BIR3/FP peptide binary complex.
Applications	The binding constants (K d) of Birinapant (TL32711) for XIAP and cIAP1 were determined to be 45 and
Cell experiment [2]:
Cell lines	451Lu and WM1366 melanoma cells
Preparation Method	Cells were treated with Birinapant (TL32711) 1 μmol/L in combination with TNF-α 1 ng/mL. Cells were then incubated for 72 hours in the presence or absence of Necrostatin-1 a RIP1 kinase inhibitor. Proliferation was assessed using the MTS assay.
Reaction Conditions	1 μmol/L Birinapant (TL32711) for 72 hours
Applications	The majority of cell lines exhibited strong combination activity of Birinapant (TL32711) and TNF-α.
Animal experiment [3]:
Animal models	Male C57BL/6J mice aged 8 week old, weighing 21 ± 1.3g
Preparation Method	Before the LPS administration, mice were injected intraperitoneally with Birinapant (TL32711) (30 mg/kg body weight, Birinapant (TL32711) group) either vehicle control (vehicle group) for 24 h. Birinapant (TL32711) was dissolved in 12.5% Captisol in distilled water. Twenty-four mice in each group were euthanized and the samples of the liver and blood were harvested at 0, 6, 12 and 24 h after LPS challleage.
Dosage form	30 mg/kg Birinapant (TL32711) ip. for 24 h.
Applications	Birinapant (TL32711) pretreatment significantly improved mice survival.
References: [1]. Allensworth JL, Sauer SJ, et,al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71. doi: 10.1007/s10549-012-2352-6. Epub 2012 Dec 7. PMID: 23225169. [2]. Krepler C, Chunduru SK, et,al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94. doi: 10.1158/1078-0432.CCR-12-2518. Epub 2013 Feb 12. PMID: 23403634; PMCID: PMC3618495. [3]. Liu H, Liao R, et,al. The SMAC mimetic birinapant attenuates lipopolysaccharide-induced liver injury by inhibiting the tumor necrosis factor receptor-associated factor 3 degradation in Kupffer cells. Immunol Lett. 2017 May;185:79-83. doi: 10.1016/j.imlet.2017.02.016. Epub 2017 Mar 9. PMID: 28286228.

Birinapant (TL32711) is a SMAC mimetic designed to specifically target cIAP1 and cIAP2 for degradation^[1]. the binding constants (K d) of Birinapant (TL32711) for XIAP and cIAP1 were determined to be 45 and^[3].

When Birinapant (TL32711) was combined with TNF-α, strong combination activity, that is, neither compound was effective individually but the combination was highly effective, was observed in 12 of 18 cell lines.Birinapant (TL32711) combined with TNF-α inhibited the growth of a melanoma cell line with acquired resistance to BRAF inhibition to the same extent as in the parental cell line^[1]. When investigated the role of Birinapant (TL32711) in radiosensitization of glioblastoma cells, Birinapant (TL32711) can enhance the radiosensitivity of glioblastoma cell lines in cell-based assays and tumor models via radiation-induced TNF-α^[4]. Combination of Birinapant (TL32711) and TNFα induced sub-G0 DNA fragmentation in sensitive lines and Birinapant (TL32711) alone also induced significant G2-M cell-cycle arrest and cell death in UM-SCC-46 cells[6]. Birinapant (TL32711) induced death receptor-/caspase-8-mediated apoptosis in AML cells, including in AML stem/progenitor cells, but not in normal CD34(+) cells^[7].

Birinapant (TL32711) significantly improved the survival rate of endotoxemic mice and attenuated LPS-induced liver pathologic damage and inflammatory response. IL-1 and TNF-α levels in the serum were markedly decreased in Birinapant (TL32711) pretreatment mice compared with control mice .The cellular inhibitor of apoptosis protein 1 (cIAP1) expression in liver resident macrophage (Kupffer cells, KCs) was significantly decreased in the Birinapant (TL32711) group compared to the Vehicle group^[2].

References:
[1]. Krepler C, Chunduru SK, et,al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94. doi: 10.1158/1078-0432.CCR-12-2518. Epub 2013 Feb 12. PMID: 23403634; PMCID: PMC3618495.
[2]. Liu H, Liao R, et,al. The SMAC mimetic birinapant attenuates lipopolysaccharide-induced liver injury by inhibiting the tumor necrosis factor receptor-associated factor 3 degradation in Kupffer cells. Immunol Lett. 2017 May;185:79-83. doi: 10.1016/j.imlet.2017.02.016. Epub 2017 Mar 9. PMID: 28286228.
[3]. Allensworth JL, Sauer SJ, et,al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71. doi: 10.1007/s10549-012-2352-6. Epub 2012 Dec 7. PMID: 23225169.
[4]. Cerna D, Lim B, A et,al.SMAC Mimetic/IAP Inhibitor Birinapant Enhances Radiosensitivity of Glioblastoma Multiforme. Radiat Res. 2021 Jun 1;195(6):549-560. doi: 10.1667/RADE-20-00171.1. PMID: 33826739.
[5]. Zhu DL, Shuai LY. Effects of Birinapant on Proliferation and Invasion of MGC-803 Gastric Cancer Cells and Mechanism Underlying These Effects. Bull Exp Biol Med. 2021 May;171(1):56-61. doi: 10.1007/s10517-021-05172-w. Epub 2021 May 29. PMID: 34050412.
[6]. Eytan DF, Snow GE, et,al. SMAC Mimetic Birinapant plus Radiation Eradicates Human Head and Neck Cancers with Genomic Amplifications of Cell Death Genes FADD and BIRC2. Cancer Res. 2016 Sep 15;76(18):5442-5454. doi: 10.1158/0008-5472.CAN-15-3317. Epub 2016 Jul 28. PMID: 27469115; PMCID: PMC5026594.
[7]. Carter BZ, Mak PY, et,al. Synergistic targeting of AML stem/progenitor cells with IAP antagonist birinapant and demethylating agents. J Natl Cancer Inst. 2014 Feb;106(2):djt440. doi: 10.1093/jnci/djt440. PMID: 24526787; PMCID: PMC3952202.

Cas No.	1260251-31-7	SDF
المرادفات	TL-32711
Chemical Name	(2S,2'S)-N,N'-((2S,2'S)-((3S,3'S,5R,5'R)-5,5'-((6,6'-difluoro-1H,1'H-[2,2'-biindole]-3,3'-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide)
Canonical 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
Formula	C₄₂H₅₆F₂N₈O₆	M.Wt	806.94
الذوبان	≥ 40.35 mg/mL in DMSO, ≥ 46.9 mg/mL in EtOH	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.2392 mL	6.1962 mL	12.3925 mL
	5 mM	0.2478 mL	1.2392 mL	2.4785 mL
	10 mM	0.1239 mL	0.6196 mL	1.2392 mL

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Birinapant (TL32711) (Synonyms: TL-32711)

مراجعات العميل

GlpBio Citations

Bioactive Compounds Premium Provider

منتجات GlpBio المذكورة في الأوراق ذات السمعة الطيبة

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

حاسبة المولارية

حاسبة التخفيف

In vivo Formulation Calculator (Clear solution)

مراجعات

Birinapant (TL32711) (Synonyms: TL-32711)

مراجعات العميل

GlpBio Citations

Bioactive Compounds Premium Provider

منتجات GlpBio المذكورة في الأوراق ذات السمعة الطيبة

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

حاسبة المولارية

حاسبة التخفيف

In vivo Formulation Calculator (Clear solution)

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