Trimetrexate

CAS No. 52128-35-5

Trimetrexate( CI-898 | NSC-249008 | CI898 | NSC249008 )

Catalog No. M14831 CAS No. 52128-35-5

A quinazoline derivative and antifolate agent that fuctions as a dihydrofolate reductase (DHFR) inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Trimetrexate
  • Note
    Research use only, not for human use.
  • Brief Description
    A quinazoline derivative and antifolate agent that fuctions as a dihydrofolate reductase (DHFR) inhibitor.
  • Description
    A quinazoline derivative and antifolate agent that fuctions as a dihydrofolate reductase (DHFR) inhibitor; shows activity against transport-deficient MTX-resistant tumor cells that overcome the acquired and natural resistance to methotrexate.Chemotherapeutic Agents Discontinued.
  • In Vitro
    Cell Proliferation Assay Cell Line:SNU-C4 and NCI-H630 Concentration:0.1 mM Incubation Time:24 h Result:Inhibited cell growth by 50-60% in both cell lines. Cell Proliferation Assay Cell Line:C4 cells Concentration:1 and 10 mM Incubation Time:24 h Result:Produced 42% and 50% lethality at 1 and 10 mM, respectively.
  • In Vivo
    Animal Model:Toxoplasma infected female BALB/c mice weighing about 20 gDosage:180 mg/kg or 30 mg/kg Administration:180 mg/kg per day orally in the drinking water or 30 mg/kg per day i.p.Result:Extended the median survival of the infected mice to 10 d (p.o.) or 19 d (i.p.).Animal Model:Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g Dosage:0, 1, 10, or 30 mg/kg Administration:Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period Result:Showed chronic toxicity, the testicular changes persisting during the course of multiple cycles of dosing were not reversible within 21 days, but required an additional 56 days for essentially complete recovery.
  • Synonyms
    CI-898 | NSC-249008 | CI898 | NSC249008
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Antifolate
  • Recptor
    Antifolate
  • Research Area
    Cancer
  • Indication
    Chemotherapeutic

Chemical Information

  • CAS Number
    52128-35-5
  • Formula Weight
    369.4176
  • Molecular Formula
    C19H23N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    NC1=NC(N)=C2C(C)=C(CNC3=CC(OC)=C(OC)C(OC)=C3)C=CC2=N1
  • Chemical Name
    2,4-Quinazolinediamine, 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-

Shipping & Storage Information

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

Reference

1. Weir EC, et al. Cancer Res. 1982 May;42(5):1696-702. 2. Diddens H, et al. Cancer Res. 1983 Nov;43(11):5286-92. 3. Elslager EF, et al. J Med Chem. 1983 Dec;26(12):1753-60. 4. Wong BK, et al. Drug Metab Dispos. 1990 Nov-Dec;18(6):980-6.
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