1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
    Apoptosis
  3. Alrizomadlin

Alrizomadlin (Synonyms: APG-115; AA-115)

目录号: HY-101518 纯度: 98.05% ee.: 100%
产品使用指南

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 Ki 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)。

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Alrizomadlin Chemical Structure

Alrizomadlin Chemical Structure

CAS No. : 1818393-16-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner[2][3].

IC50 & Target

IC50: 3.8 nm (APG-115)[1]

体外研究
(In Vitro)

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[3].
Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) enhances the anti-proliferative effect of radiotherapy at different radiation dose[3].
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[3].
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[3].
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].

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

Cell Proliferation Assay[3]

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[3]

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[3]

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[3]

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[3].

MCE 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[3]
Dosage: 100 mg/kg
Administration: Deliverer orally; once daily; 10 days
Result: Decreased xenograft tumor growth.
Clinical Trial
分子量

642.59

Formula

C34H38Cl2FN3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

纯度: 98.16%

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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
Alrizomadlin
目录号:
HY-101518
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