EHT 1610

CAS No. 1425945-60-3

EHT 1610( —— )

Catalog No. M33348 CAS No. 1425945-60-3

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    EHT 1610
  • Note
    Research use only, not for human use.
  • Brief Description
    EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively.
  • Description
    EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis-.
  • In Vitro
    Western Blot Analysis Cell Line:MHH-CALL-4 cells Concentration:0, 2.5, 5, 10 μM Incubation Time:4, 5 hours Result:Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.
  • In Vivo
    Animal Model:Xenograft models of B-ALL in mice (12-14 weeks old)Dosage:20 mg/kg Administration:Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks Result:Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.
  • Synonyms
    ——
  • Pathway
    Proteasome/Ubiquitin
  • Target
    Tyrosinase
  • Recptor
    Tyrosinase | NF-κB | GSK-3 | DYRK | CDK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1425945-60-3
  • Formula Weight
    383.4
  • Molecular Formula
    C18H14FN5O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 5 mg/mL (13.04 mM; Ultrasonic )
  • SMILES
    COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Chaikuad A, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59(22):10315-10321.?
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