1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
  3. AMG 232

AMG 232 

製品番号: HY-12296 純度: 99.90%
取扱説明書

AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

AMG 232 構造式

AMG 232 構造式

CAS 番号 : 1352066-68-2

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
5 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 228 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 780 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1200 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    AMG 232 purchased from MCE. Usage Cited in: Cell Death Discov. 2020 Jul.

    The effect of AMG-232 on the p53 signaling pathway, and the expression of IL-6 and PD-L1 at different drug doses is assessed by immunoblotting. AMG-232 treatment leads to activation of the p53 signaling pathway in the cancer cells in a dose-dependent manner. The effect of significant reduction in IL-6 expression is observed with AMG-232 in a dose-dependent manner.
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.

    IC50 & Target

    IC50: 0.6 nM (p53-MDM2 interaction)[1]
    Kd: 0.045 nM (MDM2)[1]

    体外実験

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

    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.
    体内実験

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

    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.
    臨床実験
    分子量

    568.55

    分子式

    C₂₈H₃₅Cl₂NO₅S

    CAS 番号

    1352066-68-2

    SMILES

    O=C(O)C[[email protected]]1(C)C(N([[email protected]](CS(=O)(C(C)C)=O)C(C)C)[[email protected]](C2=CC=C(Cl)C=C2)[[email protected]@H](C3=CC=CC(Cl)=C3)C1)=O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 50 mg/mL (87.94 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    参考文献

    純度: 99.90%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • モル濃度カルキュレーター

    • 希釈カルキュレーター

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    AMG 232AMG232AMG-232MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    タイトル

    お名前 *

     

    PC 用メールアドレス *

    電話番号 *

     

    勤務先/学校名 *

    Department *

     

    カスタマ需要量 *

    国会或いは地域 *

         

    必ず会社名を記載ください。個人への返信は行いません。

    メッセージ

    バルクお問い合わせ

    Inquiry Information

    製品名:
    AMG 232
    製品番号:
    HY-12296
    数量:
    MCE 日本正規代理店: