Birinapant
目录号：S7015 别名： TL32711
Molecular Weight(MW): 806.94
Birinapant是一种SMAC模拟拮抗剂，对cIAP1最有效，无细胞试验中Kd为<1 nM，对XIAP作用较弱。Phase 2。
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客户使用该产品的5个实验数据：
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Western blot from tumours harvested at day 5 after treatment showing an increase in PARP cleavage in the irinotecan-treated group.
British Journal of Cancer, 2015, 112: 1471–1479. Birinapant purchased from Selleck.
Cell survival of macrophages was measured by MTT assay after(a) 24 h and (b) 2 or 4 h posttreatment of cells with SMAC mimetic (BP, 10 μM) with or without zVAD-fmk (50 μM) or Nec-1 (10 μM). Graphs show the percentage of surviving cells relative to the corresponding vehicle control. These graphs are representative of three biological replicates each carried out in triplicate.
Cell Death Differ, 2016, 23(10):1628-37.. Birinapant purchased from Selleck.
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Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.
Cell Death Dis 2013 4, e951. Birinapant purchased from Selleck.
(a) Apoptosis assessed morphologically after DAPI staining (top panels) and by caspase 3/7 activation (bottom panels) in human cholangiocyte cell lines H69 and NHC, and the human breast cancer cell line MDA-MB-231, incubated for 24 h with or without (cnt) the SMAC mimetic TL32711 (1 μM), in the presence or absence of neutralizing antibodies against TNFα (1 μg/ml) or FasL (1 μg/ml), or recombinant TRAIL-R2:Fc (1 μg/ml).
Cell Death Dis, 2017, 8(1):e2535. Birinapant purchased from Selleck.
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FTC cell lines were treated with increasing concentrations of rh-TRAIL with and without Smac mimetics Birinapant (A/B). Changes in cell viability are illustrated linearly in percentage control and stratified according to the FP. While FTC cell line TT2609-C02 was susceptible to rh-TRAIL alone (A), cell line FTC133 proved to be resistant to rh-TRAIL induced apoptosis (B). Smac mimetic treatment alone had no impact on cell viability. Annexin-V/PI staining and FACS analyses of FTC cells demonstrate the changes of annexin positive apoptotic cells after incubation with rh-TRAIL alone (-) or in combination (+) with Smac mimetics Birinapant. Changes in protein expression of cIAP1/2 after treatment with the respective Smac mimetic are illustrated using western blot. GAPDH served as loading control. Blots are cropped to increase clarity. Statistical significance was calculated by two-tailed nonparametric Mann-Whitney test. e. survival = expected survival, sp. survival = specific survival, FP = fractional product; *p < 0.05; **p < 0.01.
Endocr Relat Cancer, 2018, 25(3):295-308. Birinapant purchased from Selleck.
产品安全说明书
IAP抑制剂选择性比较
生物活性
| 产品描述 | Birinapant是一种SMAC模拟拮抗剂，对cIAP1最有效，无细胞试验中Kd为<1 nM，对XIAP作用较弱。Phase 2。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 体外研究 |
Birinapant与XIAP和CIAP1结合的Kd分别为45 nM和 <1 nM。在TRAIL不敏感的SUM190（ErbB2的过度表达）细胞中，Birinapant独自诱导细胞死亡（IC 50约为300 nM），并显著增加TRAIL诱导的TRAIL敏感SUM149（三阴性，EGFR活化）细胞的凋亡。 Birinapant导致CIAP1迅速降解，caspase活化，PARP裂解，和NF-κB的激活。[1] Birinapant与TNF-α联用表现出强烈的体外抗黑素瘤作用。 Birinapant和TNF-α（1 ng/mL）联用抑制人黑素瘤细胞系WTH202，WM793B，WM1366和WM164生长，IC50分别为1.8，2.5，7.9和9 nM，而两种化合物单独都无效。Birinapant单独处理可诱导对WM9细胞增殖的抑制作用，IC 50为2.4 nM。Birinapant显著抑制这些细胞系中靶蛋白CIAP1和cIAP2。[2] |
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| Cell Data |
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| 体内研究 | Birinapant（30毫克/千克）显著诱导恶性黑色素瘤异种移植模型451LU的肿瘤生长。[2] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验：[1] |
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荧光偏振测定法: 和化合物XIAP和CIAP1的亲和力是使用荧光底物来确定，并以Kd值表示。最初，荧光标记的修饰的Smac肽（AbuRPF -K （5-FAM）-NH 2; FP肽）的解离常数（Kd）是用固定浓度（5 nM）的肽和滴定不同浓度的蛋白质（0.075-5μM的半对数稀释）来确定。剂量-反应曲线是在5nM FP肽和50nM XIAP检测中用GraphPad Prism的单点结合模型的非线性最小二乘法生产的。各种浓度的Smac模拟物（100-0.001 μM在半对数稀释）添加到FP肽/蛋白质二元复合物，在含有100毫克/毫升牛c-球蛋白0.1M磷酸钾缓冲液中室温处理15分钟。多标签读板器采用485 nm激发滤光片和520nm的发射滤光片测量偏振值。 |
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| 细胞实验：[2] |
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| 动物实验：[2] |
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溶解度 (25°C)
| 体外 | DMSO | 100 mg/mL (123.92 mM) |
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| Ethanol | 55 mg/mL (68.15 mM) | |
| Water | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 15% Captisol |
5 mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 806.94 |
|---|---|
| 化学式 | C42H56F2N8O6 |
| CAS号 | 1260251-31-7 |
| 稳定性 | powder |
| in solvent | |
| 别名 | TL32711 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02756130 | Withdrawn | High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma | Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) | August 1 2018 | Phase 1|Phase 2 |
| NCT02587962 | Recruiting | Solid Tumors | Medivir|Merck Sharp & Dohme Corp. | August 4 2017 | Phase 1|Phase 2 |
| NCT02288208 | Terminated | Hepatitis B | TetraLogic Pharmaceuticals | November 2014 | Phase 1 |
| NCT02147873 | Terminated | Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML) | TetraLogic Pharmaceuticals | June 2014 | Phase 2 |
| NCT01940172 | Completed | Relapsed Epithelial Ovarian Cancer|Relapsed Primary Peritoneal Cancer|Relapsed Fallopian Tube Cancer | TetraLogic Pharmaceuticals | November 2013 | Phase 1 |
| NCT01828346 | Completed | Myelodysplastic Syndrome | TetraLogic Pharmaceuticals | June 2013 | Phase 1|Phase 2 |
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