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Linsitinib

(別名: OSI-906)
51 Cited Publications
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Based on 51 publication(s) in Google Scholar

Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively.

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  • 純度: 99.90%
  • CAS 番号: 867160-71-2
  • 分子式: C26H23N5O
  • 分子量:421.49
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Linsitinib Chemical Structure
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Linsitinib Chemical Structure
    Linsitinib 構造式
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
  • Experimental Validation Results for Linsitinib
CAS 番号: 867160-71-2
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  • Linsitinib Chemical Structure
    Linsitinib Chemical Structure
    1/16
  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: Cell Metab. 2017 Apr 4;25(4):868-882.e5. [Abstract]

    Customer Validation
     Western blot of indicated proteins in control β cells in the presence of 10 nM Insulin, 200 nM OSI-906 (IR/IGF1Ri), 50μM LY294002 (PI3Ki), 5μM MK-2206 (Akti), or 20μM U0126 (MEKi) for 24 hr. Bottom: intensity of the signals quantified by densitometry.

  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jun 23;7(1):4119. [Abstract]

    Customer Validation
     Transient hyperglycemia accompanied by ephemeral hyperinsulinemia induced by IR and IGF1R inhibition with OSI-906. C57BL/6J mice are subjected to a 16-hour fast and OSI-906 (45 mg/kg) or a vehicle (Solutol HS-15) is administered orally 1 hour before injection with either saline, 10 units of insulin, or 1 mg/kg of IGF-1 via the inferior vena cava. The liver and epididymal fat are collected 70 and 120 seconds after injection, respectively.

  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2017 Dec 5;17(1):820. [Abstract]

    Customer Validation
     OSI-906 inhibits p-IGF1R and IGF1R signaling factors in breast cancer cell-lines. 3 × 105 ER-positive MCF7 and ER-negative are plated per well of a 6-well plate and cultured for 24 h and subsequently treated with the OSI-906 (0.1, 0.4 and 1.6 μM) and/or SKI-II (4 μM) for 24 h. Protein lysates are collected and 20 μg of protein is used for immunoblot analysis to measure changes to IGF1R signaling and SphK1 steady-state protein expression levels.

  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2017 Dec 5;17(1):820. [Abstract]

    Customer Validation
     OSI-906 inhibits p-IGF1R and IGF1R signaling factors in breast cancer cell-lines. HCC-1806 breast cancer cells are plated per well of a 6-well plate and cultured for 24 h and subsequently treated with OSI-906 (0.1, 0.4 and 1.6 μM) and/or SKI-II (4 μM) for 24 h. Protein lysates are collected and 20 μg of protein is used for immunoblot analysis to measure changes to IGF1R signaling and SphK1 steady-state protein expression levels.

  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: Okayama University. 2015.

    Customer Validation
     Expression of Sema4D and PlexinB1 in various oral squamous cell carcinoma cell lines following the addition of IGF-I. Notably, the addition of IGF-I resulted in increased expression of Sema4D, particularly in HSC-2 and SAS cells. This increase was suppressed when IGF-I was administered in the presence of inhibitors targeting its receptor or downstream signaling pathways. No changes in PlexinB1 expression were observed following the addition of IGF-I.

  • 1/16

    Linsitinib purchased from MedChemExpress. Usage Cited in: Endocrinology. 2014 Jun;155(6):2102-11. [Abstract]

    Customer Validation
     OSI-906 inhibits insulin receptor-mediated signaling in HEK293 cells. The cells are deprived of serum for 2 hours, stimulated for 5 min with 1 μM i nsulin in the presence or absence of 200 nM OSI-906 in serum-free medium. Cell extracts are subjected to immunoprecipitation and immunoblotting, as indicated.

  • Linsitinib