Alrizomadlin APG-115; AA-115|cas:1818393-16-6|西域试剂

Alrizomadlin APG-115; AA-115,98.05%

产品编号：Bellancom-101518| CAS NO：1818393-16-6| 分子式：C₃₄H₃₈Cl₂FN₃O₄| 分子量：642.59

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货号	价格	库存与货期
Bellancom-101518	￥3200.00	杭州北京（现货）
Bellancom-101518	￥7500.00	杭州北京（现货）
Bellancom-101518	￥12000.00	杭州北京（现货）

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Alrizomadlin APG-115; AA-115

产品介绍

Alrizomadlin (APG-115) 是一种口服活性小分子 MDM2 蛋白抑制剂, 可与 MDM2 蛋白结合，IC₅₀ 值和 K_i 值分别为3.8 nM 和 1 nM。Alrizomadlin 可阻断 MDM2 与 p53 的相互作用并且以 p53 依赖性方式诱导细胞周期停滞和凋亡 (apoptosis)。

生物活性

Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC₅₀ and K_i values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

体外研究

Alrizomadlin (0.001-100 μM; 72 hours) inhibits cell proliferation in concentration-dependent manner, with IC₅₀s of 18.9 ± 15.6 nM and 103.5 ± 18.3 nM respectively in AGS and MKN45 cells.
Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) enhances the anti-proliferative effect of radiotherapy at different radiation dose.
Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) affects progression by inducing cells arrested at G0/G1 phase in AGS and MKN45 cell with wild p53.
Alrizomadlin (0.02 μM, 0.2 μM; 24 hours) activates p53 to enhance radiosensitivity in AGS and MKN45 cells; stable knockout of p53 abrogates expression of MDM2, p53, p21, PUMA, BAX, Cleaved-caspase3, γH2AX.
Alrizomadlin (0.3 μM, 1 μM, 3 μM, 10 μM; 24 hours) leads to a concentration-dependent cell cycle arrest in G2/M phases and a decreasing in S-phase in p53 wide-type cell lines (TPC-1, KTC-1)^[4].

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

Cell Proliferation Assay

Cell Line:	AGS and MKN45 cells
Concentration:	0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation in a concentration-dependent manner.

RT-PCR

Cell Line:	AGS and MKN45 cells
Concentration:	0.02 μM, 0.2 μM
Incubation Time:	48 hours
Result:	Elevated MDM2, p21, PUMA and BAX mRNA expression.

Cell Cycle Analysis

Cell Line:	AGS and MKN45 cells
Concentration:	0.02 μM, 0.2 μM
Incubation Time:	48 hours
Result:	Arrested cells at G0/G1 phase.

Apoptosis Analysis^[4]

Cell Line:	DePTC p53 wide-type cell line: TPC-1 cells, KTC-1 cells
Concentration:	0.3μM, 1μM, 3μM, 10 μM
Incubation Time:	24 hours
Result:	Reduced cell population in S-phase, whereas accumulation of cells at G2/M phases.

Western Blot Analysis

Cell Line:	AGS and MKN45 cells
Concentration:	0.2 μM
Incubation Time:	72 hours
Result:	Enhanced expressions of MDM2 and p53, stable knockout of p53 abrogated them.

体内研究
(In Vivo)

Alrizomadlin (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo.

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

Animal Model:	Four-week-old male BALB/c athymic nude mice with MKN45 cells
Dosage:	100 mg/kg
Administration:	Deliverer orally; once daily; 10 days
Result:	Decreased xenograft tumor growth.

体内研究

Alrizomadlin (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo.

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

Animal Model:	Four-week-old male BALB/c athymic nude mice with MKN45 cells
Dosage:	100 mg/kg
Administration:	Deliverer orally; once daily; 10 days
Result:	Decreased xenograft tumor growth.

体内研究

Alrizomadlin (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo.

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

Animal Model:	Four-week-old male BALB/c athymic nude mice with MKN45 cells
Dosage:	100 mg/kg
Administration:	Deliverer orally; once daily; 10 days
Result:	Decreased xenograft tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (155.62 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5562 mL	7.7810 mL	15.5620 mL
5 mM	0.3112 mL	1.5562 mL	3.1124 mL
10 mM	0.1556 mL	0.7781 mL	1.5562 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。-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: ≥ 5 mg/mL (7.78 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (7.78 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (7.78 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.78 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。