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APG-1387
CAS No. 1570231-89-8
APG-1387 ( —— )
产品货号. M21856 CAS No. 1570231-89-8
APG-1387 是一种二价 SMAC 模拟物和 IAP 拮抗剂，可阻断 IAP 家族蛋白的活性。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥13041 | 有现货 |
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| 10MG | ￥21789 | 有现货 |
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| 100MG | 获取报价 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称APG-1387
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述APG-1387 是一种二价 SMAC 模拟物和 IAP 拮抗剂，可阻断 IAP 家族蛋白的活性。
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产品描述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.
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体外实验Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells.Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. Western Blot AnalysisCell Line:HepG2 and HCCLM3 cellsConcentration: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.
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体内实验Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice.Dasminapant (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. 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.
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同义词——
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通路Apoptosis
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靶点IAP
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受体——
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研究领域——
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适应症——
化学信息
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CAS Number1570231-89-8
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分子量1157.4
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分子式C??H??N??O??S?
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纯度>98% (HPLC)
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溶解度DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)
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SMILESO=S(C1=CC=CC(S(=O)(N(C[C@@H]2NC([C@@H](NC)C)=O)CC[C@](CC[C@H]3C(NC(C4=CC=CC=C4)C5=CC=CC=C5)=O)([H])N3C2=O)=O)=C1)(N(C[C@@H]6NC([C@@H](NC)C)=O)CC[C@](CC[C@H]7C(NC(C8=CC=CC=C8)C9=CC=CC=C9)=O)([H])N7C6=O)=O
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Chen Z, et, al. The SMAC Mimetic APG-1387 Sensitizes Immune-Mediated Cell Apoptosis in Hepatocellular Carcinoma. Front Pharmacol. 2018 Nov 6; 9:1298.
2. Li BX, et, al. Novel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, Ripoptosome and autophagy mediated cell death pathway. J Exp Clin Cancer Res. 2018 Mar 12;37(1):53.
3. Li N, et, al. A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis. Cancer Lett. 2016 Oct 10;381(1):14-22.
