| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| X409188-1ml |
1ml |
现货  |
|
| 别名 | 喜文拿潘 (AT406) |
|---|---|
| 英文别名 | ARRY-334543, Debio1143, SM-406 | (5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Xevinapant (AT406) |
| 生化机理 | Xevinapant（AT406、ARRY-334543、Debio1143、SM-406）是一种强效的Smac模拟物，也是IAP（通过E3泛素连接酶抑制凋亡蛋白）的拮抗剂，能与XIAP-BIR3、cIAP1-BIR3和cIAP2-BIR3结合，Ki分别为66.4 nM、1.9 nM和5.1 nM，比Smac AVPI肽的亲和力高50至100倍。第 1 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 含 2 的杆状病毒 IAP 重复序列拮抗剂；含 3 的杆状病毒 IAP 重复序列拮抗剂；X-连锁细胞凋亡抑制因子拮抗剂 |
| 产品介绍 |
Xevinapant (AT406, ARRY-334543, Debio1143, SM-406)是一种有效的，拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂，与XIAP-BIR3， cIAP1-BIR3和cIAP2-BIR3结合，Ki为66.4 nM， 1.9 nM和5.1 nM，比作用于Smac AVPI肽亲和力高50到100倍. Information Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) is a potent Smac mimetic and an antagonist ofIAP(inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 withKiof 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-f AT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. AT-406 is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. AT-406 (at 1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, AT-406 induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. AT-406 effectively inhibits lots of human cancer cell lines and shows IC50 of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. AT-406 induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP. In vivo AT-406 has good pharmacokinetic (PK) properties and oral bioavailability in mice, rats, non-human primates, and dogs. In the MDA-MB-231 xenograft, AT-406 effectively induces cIAP1 degradation and processing of procaspase-8, cleavage of PARP in tumor tissues at 100 mg/kg with well toleration even at 200 mg/kg. AT-406 induces significant tumor growth inhibition with p of 0.0012 at 100 mg/kg. cell lines：SW620, LoVo, V3-YAC and V3 cells Concentrations：~ 1 μM Incubation Time：4 days Powder Purity:≥99% |
| Ki Data | XIAP-BIR3, Ki: 66.4 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CNC(C)C(=O)NC1CN(CCC2CCC(N2C1=O)C(=O)NC(C3=CC=CC=C3)C4=CC=CC=C4)C(=O)CC(C)C |
| 分子量 | 561.71 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 64 mg/mL (200.08 mM); Ethanol: 64 mg/mL (200.08 mM); Water: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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