1. Protein Tyrosine Kinase/RTK
  2. Insulin Receptor

NT157 (Synonyms: Tyrphostin NT157)

Cat. No.: HY-100037 Purity: 99.19%
Handling Instructions

NT157is a selective inhibitor of IRS-1/2, IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) .

For research use only. We do not sell to patients.

NT157 Chemical Structure

NT157 Chemical Structure

CAS No. : 1384426-12-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 190 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
2 mg USD 110 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 310 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
25 mg USD 600 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    NT157 purchased from MCE. Usage Cited in: Nat Commun. 2018 Jul 4;9(1):2611.

    Western blot of Gr-1+CD11b+myeloid cells collected from spleen of 4T1 tumor-bearing mice treated with NT157 (n=5).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    NT157is a selective inhibitor of IRS-1/2, IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) . IC50 value: 0.3 to 0.8 μM [1] Target: Insulin receptor in vitro: NT157 significantly affects the cells' migratory ability, as confirmed by a wound-healing assay. NT157 induces cytostatic effects, as evidenced by G2/M cell cycle arrest, and does not affect apoptosis. NT157, a novel small-molecule that specifically targets IRS protein, in OS cells. NT157 is a small-molecule inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1 and IRS-2. NT157 efficiently affects migration ability of MG-63 and U-2OS OS cells. NT157 treatment induces cell cycle arrest and inhibits IGF system signaling. [1] The density of LNCaP cells grown in FBS was decreased approximately 20% at 1 μM, approximately 70% at 2 μM, and >90% at 5 μM (IC50, 1.4 μM). Growth of LNCaP cells is suppressed >60% when cultured in CSS but still exhibited significant density at 2 μM and maximal decreased density at 5 μM. The density of FBS-cultured PC3 cells was similarly decreased by NT157 treatment (40% at 2 μM and > 70% at 5 μM; IC50, 2.5 μM). [2] in vivo: NT157 suppresses growth of LNCaP xenografts following castration. NT157 treatment affects IGF1R and IRS targets in xenografts and significantly delays castration-resistant progression of LNCaP androgen-responsive xenografts when combined with castration. NT157 potentiates docetaxel activity in PC3 xenografts.[2]

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (72.77 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4257 mL 12.1283 mL 24.2565 mL
    5 mM 0.4851 mL 2.4257 mL 4.8513 mL
    10 mM 0.2426 mL 1.2128 mL 2.4257 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      NT157 is dissolved in 20% 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD)[3].

       
    References
    Molecular Weight

    412.26

    Formula

    C₁₆H₁₄BrNO₅S

    CAS No.

    1384426-12-3

    SMILES

    S=C(NCC1=CC(O)=C(O)C(O)=C1)/C=C/C2=CC(O)=C(O)C(Br)=C2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.19%

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    Product Name:
    NT157
    Cat. No.:
    HY-100037
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    NT157

    Cat. No.: HY-100037