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CB1954

Cat. No. M5482
CB1954 Structure
Synonym:

Tretazicar

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 85  USD85 In stock
25mg USD 175  USD175 In stock
50mg USD 265  USD265 In stock
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Quality Control & Documentation
Biological Activity

CB1954(Tretazicar) is a anticancer 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. It can be activated by NAD(P)H quinone oxidoreductase 2.

Chemical Information
Molecular Weight 252.18
Formula C9H8N4O5
CAS Number 21919-05-1
Solubility (25°C) 50 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Teng G, et al, Mol Med Rep. Combined antitumor activity of the nitroreductase/CB1954 suicide gene system and γ-rays in HeLa cells in vitro.

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Keywords: CB1954, Tretazicar supplier, inhibitors, activators


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