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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Apoptosis > BirinapantCAS：1260251-31-7
Molecular Formula：C42H56F2N8O6
Molecular Weight：806.94
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to yellow Solid
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| CAS | 1260251-31-7 |
| Name | Birinapant |
| Molecular Formula | C42H56F2N8O6 |
| Molecular Weight | 806.94 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25976869 |
| SMILES | FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2 |
| Target Point | Apoptosis;IAP |
| Passage | Apoptosis |
| Background | Birinapant is a potent antagonist of XIAP and cIAP1. |
| Biological Activity | Birinapant是一种二价Smac模拟物， 是 XIAP 和 cIAP1 的强效拮抗剂，Kd 值分别为45 nM和小于1 nM[1-3]。 |
| In Vitro | Birinapant引起cIAP1和2的显著降解。在处理4小时内，Birinapant + TRAIL处理的细胞显示活性caspase-8和caspase-3水平以及PARP裂解超过单一药物，表明凋亡介导的细胞死亡。 Birinapan以剂量依赖性方式显著降低SUM190细胞的活力。在XIAP敲低细胞系(SUM190 shXIAP)中的Birinapant处理导致在较低剂量(30-300nM)下整体降低活力[1]。 Birinapant在敏感细胞中引起细胞凋亡。 Birinapant与TNF-α结合，导致451Lu和WM1366细胞系PARP裂解[2]。 Birinapant诱导HCT116人结肠癌和MDA-MB-231人乳腺癌细胞中caspase-3活化的时间过程[3]。 |
| In Vivo | Birinapant可抑制黑色素瘤异种移植模型中的肿瘤生长。在相同肿瘤的活组织检查中活化的胱天蛋白酶-3的染色显示在birinapant处理的动物中凋亡细胞适度增加[2]。 Birinapant(15 mg/kg，ip)诱导HCT116荷瘤小鼠细胞凋亡[3]。 |
| Cell Experiment | 如所述进行台盼蓝排除测定。将细胞以每孔7.5×10 4(SUM149)或1.5×105(SUM190)细胞接种于6孔板中，并使其粘附过夜。细胞用TRAIL(0-100 ng/mL)，Birinapant(0-10，000 nM)，GT13402(0-10，000 nM)，TNF-α(50 ng/mL)，TNF-α中和抗体(10μg/ mL)处理)，泛半胱天冬酶抑制剂Q-VD-OPh(20μM)，或所示的组合。所有处理均施用24小时，然后将细胞用胰蛋白酶消化并重悬于PBS中。接下来，将10μL细胞悬浮液加入到10μL0.4％台盼蓝中，并将10μL混合物加载到血细胞计数器上;计数细胞，记录活细胞数和死细胞数。 |
| Animal Experiment | 将10只动物各自用1×106 451Lu或1205Lu人黑素瘤细胞皮下接种于基质胶/完全培养基的悬浮液中，比例为1：1。在形成可触知的肿瘤后，将来自两种肿瘤模型的小鼠随机分成两组。两组均用载体对照或birinapant 30mg/kg腹膜内注射三次/周，持续21天。将Birinapant溶于蒸馏水中的12.5％Captisol中。通过卡尺测量每周评估肿瘤大小两次。随后，分别以451Lu和1205Lu肿瘤细胞以相同的方式接种10只和15只小鼠的卫星组。在肿瘤达到200mm 3的平均体积后，如上所述给动物服用birinapant或载体对照。在48小时和两个剂量后，处死动物并在最后一次处理后的四个时间点收获肿瘤。将肿瘤样品在液氮中快速冷冻用于随后的蛋白质分析，并保存为用于免疫组织化学的FFPE块。 |
| Data Literature Source | [1]. Allensworth JL，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. [2]. Krepler C，et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94. [3]. Nguyen QD，et al. Temporal and spatial evolution of therapy-induced tumor apoptosis detected by caspase-3-selective molecular imaging. Clin Cancer Res. 2013 Jul 15;19(14):3914-24. |
| Unit | Bottle |
| Specification | 5mg 10mg |
Birinapant是 XIAP 和 cIAP1 的强效拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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