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

Idasanutlin (Synonyms: RG7388)

製品番号: HY-15676 純度: 99.90%
取扱説明書

Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.

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Idasanutlin 構造式

Idasanutlin 構造式

CAS 番号 : 1229705-06-9

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  
10 mM * 1 mL in DMSO USD 95 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 290 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 490 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 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Idasanutlin purchased from MCE. Usage Cited in: Preprints. 2018, 2018100121.

    Effect of SAHA and RG7388 treatments on Cell Cycle related Protein levels in MCF-7 cells. Figure shows upregulation of p21, p27, AURKB and CDC25C levels after treatment with 7.5 µM concentration of SAHA and p53 upregulation after RG7388 treatment.

    Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8.

    Modulation of apoptosis-related protein expressions in MCF-7 cells after SAHA (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h.

    Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8.

    Modulation of necroptosis-related protein expressions in MCF-7 cells after (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h

    Idasanutlin purchased from MCE. Usage Cited in: Cancer Res. 2019 May 1;79(9):2404-2414.

    Immunoblot for p53 pathway responses to 壹dasanutlin treatment (1 μM for 24h) in TTC642 cells reexpressing SMARCB1. Images are representative of three biological replicates.
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    製品説明

    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.

    IC50 & Target

    IC50: 6 nM (p53-MDM2)[1]

    体外実験

    Idasanutlin (RG7388) inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53[1]. Idasanutlin (RG7388) (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells[2].

    体内実験

    Idasanutlin (RG7388, 25 mg/kg p.o.) results in tumor growth inhibition and regression, in the mouse SJSA human osteosarcoma xenograft model[1]. Idasanutlin (RG7388) induces induction of apoptosis and antiproliferation, in the SJSA xenograft model[2].

    臨床実験
    分子量

    616.48

    分子式

    C₃₁H₂₉Cl₂F₂N₃O₄

    CAS 番号

    1229705-06-9

    SMILES

    O=C(O)C1=CC(OC)=C(NC([[email protected]]2[[email protected]](C3=C(F)C(Cl)=CC=C3)[[email protected]](C4=CC=C(Cl)C=C4F)(C#N)[[email protected]](CC(C)(C)C)N2)=O)C=C1

    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
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 45 mg/mL (73.00 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6221 mL 8.1106 mL 16.2211 mL
    5 mM 0.3244 mL 1.6221 mL 3.2442 mL
    10 mM 0.1622 mL 0.8111 mL 1.6221 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [1]

    Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [2]

    At 10 to 12 weeks of age, mice are implanted with a 1:1 mixture of human SJSA osteosarcoma cells (ATCC) suspended in phenol-free Matrigel and PBS. Mice are implanted in the right flank at a concentration of 5×106 cells in 0.2 mL total volume. At approximately day 10, animals are randomized according to tumor volume, so that all groups of 10 randomized mice have similar starting mean tumor volumes of 100 to 250 mm3. Idasanutlin (RG7388) is administered as an amorphous solid dispersion microbulk precipitate powder containing 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer that is reconstituted immediately before administration as a suspension in Klucel/Tween, and remaining suspension is discarded after dosing.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.90%

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    The molarity calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Keywords:

    IdasanutlinRG7388RG 7388RG-7388MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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    製品名:
    Idasanutlin
    製品番号:
    HY-15676
    数量:
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