Tretazicar

SKU: orb1222509

Description

Tretazicar (CB1954) is a dinitrobenzamide prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. CB1954 has been proposed for use in enzyme-prodrug gene therapy systems with the Escherichia coli enzyme nitroreductase (Ntr). Ntr converts CB1954 to 2- and 4-hydroxylamino derivatives, whereupon the non-enzymatic reaction of the 4-hydroxylamino derivative with cellular thio- esters generates a potent cytotoxic bifunctional alkylating agent capable of cross-linking DNA.

Key Properties

• CAS Number: 21919-05-1
• MW: 252.18
• Purity: >98% (HPLC)
• Formula: C₉H₈N₄O₅
• SMILES: NC(=O)c1c(cc(c(c1)N1CC1)[N+](=O)[O-])[N+](=O)[O-]
• Target: mTOR
• Solubility: In Vitro: DMSO : 125 mg/mL (495.68 mM)

Bioactivity

• In Vivo:
  Animal model: Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft). Dosage: 80 mg/kg. Administration: i.p. on days 2 and 9. Result: The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CB1954 | CB-1954 | CB 1954 | Tretazicar

Quick Database Links

Gene Symbol

mTOR