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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.

Images & Validation

Key Properties

CAS Number21919-05-1
MW252.18
Purity>98% (HPLC)
FormulaC9H8N4O5
SMILESNC(=O)c1c(cc(c(c1)N1CC1)[N+](=O)[O-])[N+](=O)[O-]
TargetmTOR
SolubilityIn 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CB1954 | CB-1954 | CB 1954 | Tretazicar

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Tretazicar (orb1222509)

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Available Sizes

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100 mg
200 mg
500 mg
5 mg
¥ 1,170.00
10 mg
¥ 1,690.00
25 mg
¥ 2,860.00
50 mg
¥ 4,160.00