1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. LY3214996

LY3214996 

製品番号: HY-101494 純度: 99.54%
取扱説明書

LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.

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LY3214996 構造式

LY3214996 構造式

CAS 番号 : 1951483-29-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 239 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 80 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 240 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 380 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1300 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2100 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 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LY3214996 purchased from MCE. Usage Cited in: Cancer Sci. 2019 May;110(5):1746-1759.

    Cells are treated with RA in the presence or absence of the Erk1/2 inhibitor LY3214996, phospho-Erk1/2, Erk1/2, phospho-JNK, JNK, phospho-c-Jun, c-Jun, total and cleaved PARP, phospho-STAT3S727, and STAT3 are analyzed.

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    製品説明

    LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.

    IC50 & Target[1]

    ERK1

    5 nM (IC50)

    ERK2

    5 nM (IC50)

    体外実験

    LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996[1].

    体内実験

    In tumor xenograft models, LY3214996 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. LY3214996 shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent LY3214996 significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, LY3214996 can be tailored for treatment of cancers with MAPK pathway alteration. In addition, LY3214996 has anti-tumor activity in a Vemurafenib-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, LY3214996 can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of LY3214996 and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers[1].

    臨床実験
    分子量

    453.56

    分子式

    C₂₂H₂₇N₇O₂S

    CAS 番号

    1951483-29-6

    SMILES

    O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5

    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 : 20 mg/mL (44.10 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2048 mL 11.0239 mL 22.0478 mL
    5 mM 0.4410 mL 2.2048 mL 4.4096 mL
    10 mM 0.2205 mL 1.1024 mL 2.2048 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 mg/mL (4.41 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2 mg/mL (4.41 mM); Clear solution

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

    LY3214996LY 3214996LY-3214996ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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    製品名:
    LY3214996
    製品番号:
    HY-101494
    数量:
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