Navtemadlin(Synonyms: AMG 232; KRT-232)

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Navtemadlin (Synonyms: AMG 232; KRT-232) 纯度: 99.43%

Navtemadlin (AMG 232) 是一种有效，选择性，可口服的 p53-MDM2 相互作用抑制剂，IC50 值为 0.6 nM，与 MDM2 结合的 Kd 为 0.045 nM。

Navtemadlin(Synonyms: AMG 232; KRT-232)

Navtemadlin Chemical Structure

CAS No. : 1352066-68-2

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Navtemadlin 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Peptidomimetic Library

生物活性

Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].

IC50 & Target

IC50: 0.6 nM (p53-MDM2 interaction)[1]
Kd: 0.045 nM (MDM2)[1]
体外研究
(In Vitro)

Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines[1].
Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.
Concentration: 0-10 μM.
Incubation Time: 72 hours.
Result: Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN).
Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.

体内研究
(In Vivo)

Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo[1].
Navtemadlin causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (n=10/group) based cancer models[1].
Dosage: 10, 25, 75 mg/kg.
Administration: Once daily by oral gavage.
Result: Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED50 of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

Clinical Trial

分子量

568.55

Formula

C28H35Cl2NO5S
CAS 号

1352066-68-2
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

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (87.94 mM)

H2O : ≥ 0.1 mg/mL (0.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7589 mL 8.7943 mL 17.5886 mL
5 mM 0.3518 mL 1.7589 mL 3.5177 mL
10 mM 0.1759 mL 0.8794 mL 1.7589 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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： 50% PEG300    50% saline

    Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.40 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

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.40 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。

  • 4.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

  • 5.

    请依序添加每种溶剂： PBS

    Solubility: 1.5 mg/mL (2.64 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58.

    [2]. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41.

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