CB1954(Tretazicar)

  Cat. No.:  DC9743   Featured
Chemical Structure
21919-05-1
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Field of application
Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involve
Cas No.: 21919-05-1
Chemical Name: CB 1954,CB-1954
Synonyms: CB 1954,CB-1954
SMILES: O=[N+]([O-])C(C=C1[N+]([O-])=O)=C(C=C1C(N)=O)N2CC2
Formula: C9H8N4O5
M.Wt: 252.18
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)[1][2].
In Vivo: Tretazicar (CB 1954) (80 mg/kg; i.p. on days 2 and 9) results in a significant increase in survival[3]. Animal Model: Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)[3] 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.
In Vitro: Tretazicar (CB 1954) (0.1-1000 μM; 3 days) has sensitivity for retrovirally transduced AB22 (AB22-nr) cells with an IC50 of 3 μM[3]. DNA cross-link formation in affected cells is a result of the bioactivation of the drug by the enzyme DT diaphorase (NAD(P)H dehydro-genase (quinone)) in the Walker cells which reduces the 4-nitro group of Tretazicar. The product of this reaction is a difunctional alkylating agent, 5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide[4].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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