ホームページ Apoptosis IAP antagonist - HIV inhibitor - Apoptosis related activator Birinapant For research use only.

Birinapant

別名：TL32711

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.

Birinapant化学構造

CAS No. 1260251-31-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 70500 国内在庫あり
JPY 55500 国内在庫なし(納期7~10日)
JPY 145500 国内在庫あり
JPY 670500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Birinapantと併用されることが多い化合物

Zosuquidar 3HCl

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

Morrish E, et al. Viruses. 2020 Aug 17;12(8):901.

Birinapant関連製品

シグナル伝達経路

IAP Signaling Pathways

IAPシグナル伝達経路

IAP阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Molm13  Function Assay 2/20/200 nM 24 h decreases cIAP1 and, to a much lesser extent, cIAP2, and XIAP under various conditions 24526787
PANC-1 Growth Inhibition Assay 50/200/500 nM 0-96 h inhibits cell growth in both time and dose dependent manner 26252969
WM1366 Growth Inhibition Assay 72 h IC50=7.9 nM, combined with 1ng/ml TNF-α 23403634
WM9 Growth Inhibition Assay 72 h IC50=2.7 nM, combined with 1ng/ml TNF-α 23403634
WM9 Growth Inhibition Assay 72 h IC50=2.4 nM 23403634
WM793B Growth Inhibition Assay 72 h IC50=2.5 nM, combined with 1ng/ml TNF-α 23403634
WTH202 Growth Inhibition Assay 72 h IC50=1.8 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
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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.
Targets
cIAP1 [1]
(Cell-free assay)		 XIAP [1]
(Cell-free assay)
<1 nM(Kd) 45 nM(Kd)
In Vitro
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]
Kinase Assay 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.
細胞実験 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
実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. [2]
動物実験 動物モデル Human melanoma xenografts 451Lu
投与量 30 mg/kg
投与経路 3 times per week intraperitoneally
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

化学情報

分子量 806.94 化学式

C42H56F2N8O6
CAS No. 1260251-31-7 SDF Download Birinapant SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (123.92 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 55 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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