产品
编 号：F099712
分子式：C42H56F2N8O6
分子量：806.94
分子式：C42H56F2N8O6
分子量：806.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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2mg
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5mg
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10mg
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50mg
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结构图
CAS No: 1260251-31-7
产品详情
生物活性：
Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
体内研究：
Birinapant (TL32711) (30 mg/kg；腹腔注射；每三天 (*5)) 显示出抗肿瘤功效，并且在临床前模型中没有明显的毒性。Animal Model:Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma)
Dosage:30 mg/kg
Administration:Intraperitoneal injection; every third day (*5)
Result:Resulted in inhibition of tumor growth.
体外研究：
Birinapant (TL32711) (30-10000 nM；24 小时) 以剂量依赖性方式显著降低 SUM190 细胞的活力。Birinapant (TL32711) (30-1000 nM；4 小时) 显示 cIAP1 水平显著降低和 PARP 裂解增强，并诱导细胞凋亡。Birinapant (TL32711) 以高亲和力结合 cIAP1 的分离 BIR3 结构域，cIAP2、XIAP 和 ML-IAP 的单个 BIR 结构域可快速降解 TRAF2 结合的 cIAP1 和 cIAP2，从而抑制 TNF 介导的 NF-κB 激活。
Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
体内研究：
Birinapant (TL32711) (30 mg/kg；腹腔注射；每三天 (*5)) 显示出抗肿瘤功效，并且在临床前模型中没有明显的毒性。Animal Model:Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma)
Dosage:30 mg/kg
Administration:Intraperitoneal injection; every third day (*5)
Result:Resulted in inhibition of tumor growth.
体外研究：
Birinapant (TL32711) (30-10000 nM；24 小时) 以剂量依赖性方式显著降低 SUM190 细胞的活力。Birinapant (TL32711) (30-1000 nM；4 小时) 显示 cIAP1 水平显著降低和 PARP 裂解增强，并诱导细胞凋亡。Birinapant (TL32711) 以高亲和力结合 cIAP1 的分离 BIR3 结构域，cIAP2、XIAP 和 ML-IAP 的单个 BIR 结构域可快速降解 TRAF2 结合的 cIAP1 和 cIAP2，从而抑制 TNF 介导的 NF-κB 激活。
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