计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存,充氩。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1 , cIAP-2 , and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis . APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer , and nasopharyngeal carcinoma
In Vitro
APG-1387 (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells. APG-1387 (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. APG-1387 sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HepG2 and HCCLM3 cells Concentration: 0.02, 0.2, 2, 20 μM Incubation Time: 1, 6, 24 hours Result: Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner. Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.
In Vivo
APG-1387 (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice . APG-1387 (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells Dosage: 20 mg/kg Administration: I.p. every 3 days for 4 weeks Result: Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression. Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.
Form:Solid
IC50& Target:IAP
规格
规格或纯度
≥99%
英文名称
APG-1387
生化机理
APG-1387 是一种二价 SMAC 拟效物和 IAP 拮抗剂，可阻断 IAPs 家族蛋白（XIAP、cIAP-1、cIAP-2 和 ML-IAP）的活性。APG-1387 可诱导 cIAP-1 和 XIAP 蛋白的降解，以及 caspase-3 的活化和 PARP 的裂解。
储存条件
-20°C储存,充氩
运输条件
超低温运输
作用类型
拮抗剂
纯度
≥99%
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@@H](C(=O)N[C@H]1CN(CC[C@H]2CC[C@H](N2C1=O)C(=O)NC(C3=CC=CC=C3)C4=CC=CC=C4)S(=O)(=O)C5=CC(=CC=C5)S(=O)(=O)N6CC[C@H]7CC[C@H](N7C(=O)[C@H](C6)NC(=O)[C@H](C)NC)C(=O)NC(C8=CC=CC=C8)C9=CC=CC=C9)NC
PubChem CID
分子量
1157.40
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 50 mg/mL (43.20 mM; Need ultrasonic) H2O : <0.1 mg/mL (insoluble)
分子量
1157.400 g/mol
XLogP3
4.500
氢键供体数Hydrogen Bond Donor Count
6
氢键受体数Hydrogen Bond Acceptor Count
14
可旋转键计数Rotatable Bond Count
18
精确质量Exact Mass
1156.49 Da
单同位素质量Monoisotopic Mass
1156.49 Da
拓扑极表面积Topological Polar Surface Area
273.000 Ų
重原子数Heavy Atom Count
82
形式电荷Formal Charge
0
复杂度Complexity
2240.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
8
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
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