APG-1387|cas:1570231-89-8|西域试剂

APG-1387,99.46%

产品编号：Bellancom-125593| CAS NO：1570231-89-8| 分子式：C₆₀H₇₂N₁₀O₁₀S₂| 分子量：1157.40

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货号	价格	库存与货期
Bellancom-125593	￥6500.00	杭州北京（现货）
Bellancom-125593	￥19500.00	杭州北京（现货）
Bellancom-125593	￥32500.00	杭州北京（现货）

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APG-1387

产品介绍

APG-1387 是一种二价 SMAC 模拟物，是 IAP 拮抗剂，可阻断 IAP 家族蛋白 (XIAP，cIAP-1，cIAP-2 和 ML-IAP) 的活性。APG-1387 诱导 cIAP-1 和 XIAP 蛋白降解以及 caspase-3 激活和 PARP 裂解，从而导致细胞凋亡。APG-1387 可用于肝细胞癌，卵巢癌和鼻咽癌的研究。

生物活性

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^[4]^[5].

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell 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.

体内研究
(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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8640 mL	4.3200 mL	8.6401 mL
5 mM	0.1728 mL	0.8640 mL	1.7280 mL
10 mM	0.0864 mL	0.4320 mL	0.8640 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (2.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (2.16 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (2.16 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。