GLPBio

Birinapant (TL32711)

Catalog No.: GC12426Purity:>99.50%Synonyms: TL-32711
COASDSData Sheet

مضاد لـ cIAP1 و cIAP2 و XIAP

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

Birinapant (TL32711)
Cas No.: 1260251-31-7
10mM (in 1mL DMSO)In Stock
$93.00
1
5mgIn Stock
$65.00
1
10mgIn Stock
$104.00
1
25mgIn Stock
$165.00
1
50mgIn Stock
$237.00
1
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المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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الوصف (Description)

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.

البروتوكول (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.

وثائق المنتج (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1260251-31-7
المرادفات
TL-32711
الاسم الكيميائي
(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)
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
الصيغة الجزيئية
C42H56F2N8O6
الوزن الجزيئي
806.94
الذوبانية
≥ 40.35 mg/mL in DMSO, ≥ 46.9 mg/mL in EtOH
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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