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Home - Products - Cell Cycle/DNA Damage - DNA Alkylator - OBI-3424

OBI-3424

CAS No. 2097713-68-1

OBI-3424( AST-3424 | TH-3424 )

Catalog No. M13309 CAS No. 2097713-68-1

OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    OBI-3424
  • Note
    Research use only, not for human use.
  • Brief Description
    OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.
  • Description
    OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent; OBI-3424 is a nitro-benzene prodrug of N,N’-bisethylenephosphoramidate, demonstrates in vivo efficacy against preclinical xenograft models of pediatric T-ALL.Liver Cancer Phase 2 Clinical.
  • In Vitro
    OBI-3424 exerts potent cytotoxicity against the H460 lung cancer cell line (IC50 of 4.0 nM). OBI-3424 exhibits potent cytotoxicity, in particular against cell lines derived from T-ALL with high AKR1C3 expression, with IC50 values in the low nM range.OBI-3424 also exerts potent cell killing against ALL PDXs, and the median IC50 values were 60.3 nM for B-ALL, 9.7 nM for T-ALL and 31.5 nM for ETP-ALL.
  • In Vivo
    OBI-3424 (0.5-2.5 mg/kg; i.p.; once weekly; for 3 weeks) treatment induces regressions in PDXs mice and results in prolongation of mouse event-free survival. Animal Model:Female NSG mice (20-25 g) bearing patient-derived xenografts (PDX)Dosage:0.5 mg/kg, 1 mg/kg, 2.5 mg/kg Administration:Intraperitoneal injection; once weekly; for 3 weeks Result:Resulted in prolongation of mouse event-free survival.
  • Synonyms
    AST-3424 | TH-3424
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    DNA Alkylator
  • Recptor
    DNA Alkylator
  • Research Area
    Cancer
  • Indication
    Liver Cancer

Chemical Information

  • CAS Number
    2097713-68-1
  • Formula Weight
    460.427
  • Molecular Formula
    C21H25N4O6P
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (108.60 mM)
  • SMILES
    CC(C1=CC(=C(C=C1)[N+](=O)[O-])OC2=CC=CC(=C2)C(=O)N(C)C)OP(=O)(N3CC3)N4CC4
  • Chemical Name
    (R)-1-(3-(3-(dimethylcarbamoyl)phenoxy)-4-nitrophenyl)ethyl di(aziridin-1-yl)phosphinate

Shipping & Storage Information

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

Reference

1. Richard B. Lock, et al. Abstract LB-B16: The AKR1C3-Activated Prodrug OBI-3424 Exerts Profound In Vivo Efficacy Against Preclinical Models of T-Cell Acute Lymphoblastic Leukemia (T-ALL); a Pediatric Preclinical Testing Consortium Study. AACR 2018.
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