Birinapant (TL32711)

製品コードS7015 バッチS701504

印刷

化学情報

Chemical Structure Synonyms TL32711 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C42H56F2N8O6
分子量 806.94 CAS No. 1260251-31-7
Solubility (25°C)* 体外 DMSO 100 mg/mL (123.92 mM)
Ethanol 100 mg/mL (123.92 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
in vitro Birinapant binds with XIAP and cIAP1 with Kd 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. [1] 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.[2]
in vivo Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. [2]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Human melanoma cell lines WM9
濃度 1 nM-1 μM
反応時間 3 days
実験の流れ 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
動物実験 動物モデル Human melanoma xenografts 451Lu
投薬量 30 mg/kg
投与方法 3 times per week intraperitoneally

参考

  • https://pubmed.ncbi.nlm.nih.gov/23225169/
  • https://pubmed.ncbi.nlm.nih.gov/23403634/

カスタマーフィードバック

Data from [Cell Death Dis, 2013, 4, e951]

Data from [Data independently produced by , , British Journal of Cancer, 2015, 112: 1471–1479]

Data from [Data independently produced by , , Cell Death Differ, 2016, 23(10):1628-37.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Inhibition of heme biosynthesis triggers cuproptosis in acute myeloid leukemia [ Cell, 2025, S0092-8674(25)01233-4] PubMed: 41265435
Targeting cIAP2 in a novel senolytic strategy prevents glioblastoma recurrence after radiotherapy [ EMBO Mol Med, 2025, 10.1038/s44321-025-00201-x] PubMed: 39972068
Necrosis drives susceptibility to Mycobacterium tuberculosis in PolgD257A mutator mice [ Infect Immun, 2025, 93(3):e0032424] PubMed: 39969190
Heterogeneity-driven phenotypic plasticity and treatment response in branched-organoid models of pancreatic ductal adenocarcinoma [ Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9] PubMed: 39658630
EGFR inhibits TNF-α-mediated pathway by phosphorylating TNFR1 at tyrosine 360 and 401 [ Cell Death Differ, 2024, 31(10):1318-1332] PubMed: 38789573
EGFR inhibits TNF-α-mediated pathway by phosphorylating TNFR1 at tyrosine 360 and 401 [ Cell Death Differ, 2024, 10.1038/s41418-024-01316-3] PubMed: 38789573
Human 3D Ovarian Cancer Models Reveal Malignant Cell-Intrinsic and -Extrinsic Factors That Influence CAR T-cell Activity [ Cancer Res, 2024, 84(15):2432-2449] PubMed: 38819641
Combination of bazedoxifene with chemotherapy and SMAC-mimetics for the treatment of colorectal cancer [ Cell Death Dis, 2024, 15(4):255] PubMed: 38600086
LUBAC-mediated M1 Ub regulates necroptosis by segregating the cellular distribution of active MLKL [ Cell Death Dis, 2024, 15(1):77] PubMed: 38245534
IRE1 RNase controls CD95-mediated cell death [ EMBO Rep, 2024, 25(4):1792-1813] PubMed: 38383861

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。