STAT3-IN-13

CAS No. 2248552-86-3

STAT3-IN-13( —— )

Catalog No. M35646 CAS No. 2248552-86-3

STAT3-IN-13 is a potent STAT3 inhibitor.STAT3-IN-13 has antiproliferative and anticancer activity and acts by binding to the structural domain of STAT3 SH2.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    STAT3-IN-13
  • Note
    Research use only, not for human use.
  • Brief Description
    STAT3-IN-13 is a potent STAT3 inhibitor.STAT3-IN-13 has antiproliferative and anticancer activity and acts by binding to the structural domain of STAT3 SH2.
  • Description
    STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research.
  • In Vitro
    STAT3-IN-13 (compound 6f) (48 hours) has anti-proliferative activity with IC50 values of 0.25, 0.11 and 0.55 μM for 143B, HOS and MG63 cells, respectively.STAT3-IN-13 (compound 6f) (0.001-100 μM) binds to STAT3 and interacts with STAT3586?685 in a concentration dependent manner with a KD of 0.96 μM.STAT3-IN-13 (compound 6f) (0-1.0 μM; 24 hours; 143B and HOS cells) inhibits STAT3 Y705 phosphorylation and suppresses STAT3 in tumor cells.STAT3-IN-13 (compound 6f) (0-1.0 μM; 48 hours; 143B cells) induces apoptosis in a dose-dependent manner.Apoptosis Analysis Cell Line:143B cells Concentration:0, 0.2, 0.5, and 1 μM Incubation Time:48 hours Result:Increased the percentage of apoptosis rates of 3.4%, 8.7%, 10.7%, and 23.3% at 0, 0.2, 0.5 and 1 μM, respectively. Western Blot Analysis Cell Line:143B and HOS cells Concentration:0, 0.2, 0.5 and 1.0 μM Incubation Time:24 hours Result:Inhibited STAT3 Y705 phosphorylation and downstream target gene expression including Bcl-2 and VEGF, retained good antitumor activities against control tumor cells without STAT3 knockdown.
  • In Vivo
    STAT3-IN-13 (compound 6f) (10-20 mg/kg; i.p.; twice daily, for 4 weeks; nude mice) blocks osteosarcoma growth and metastasis in vivo.Animal Model:Nude mice Dosage:10 and 20 mg/kg Administration:Intraperitoneal injection; twice daily, for 4 weeks Result:Suppressed tumor weight at a dose of 10 mg/kg.
  • Synonyms
    ——
  • Pathway
    JAK/STAT Signaling
  • Target
    STAT
  • Recptor
    STAT
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2248552-86-3
  • Formula Weight
    436.49
  • Molecular Formula
    C21H20N6O3S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (286.38 mM; Ultrasonic )
  • SMILES
    C(#N)C=1C2=C(SC1NC(=O)C=3C=NN(C)C3)CN(C(NC4=CC=C(OC)C=C4)=O)CC2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Jin W, et, al. Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis. J Med Chem. 2022 May 12;65(9):6710-6728. ?
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