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TAS-103 dihydrochloride

Cat. No. M3725
TAS-103 dihydrochloride Structure
Synonym:

BMS-247615

Size Price Availability Quantity
5mg USD 108  USD108 In stock
10mg USD 160  USD160 In stock
25mg USD 345  USD345 In stock
50mg USD 515  USD515 In stock
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Quality Control & Documentation
Biological Activity

TAS-103 has been reported to be a potent topoisomerase II poison. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05). The combination with CDDP augmented the antitumor activity of TAS-103 (p<0.05), indicating that CDDP is one of the most potent candidates to be used in combination with TAS-103. TAS-103 may be useful in the chemotherapy of colorectal cancer. TAS-103 is a novel type of anticancer agent with a unique mechanism and could be useful as a lead compound for development of new drugs.TAS-103 will be expected to show excellent antitumor activities against a wide range of human tumors. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05).

Chemical Information
Molecular Weight 406.31
Formula C20H21Cl2N3O2
CAS Number 174634-09-4
Solubility (25°C) Water 40 mg/mL
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] Fujimoto S. Biol Pharm Bull. Promising antitumor activity of a novel quinoline derivative, TAS-103, against fresh clinical specimens of eight types of tumors measured by flow cytometric DNA analysis.

[2] Tsunoda T, et al. Anticancer Res. In vitro antitumor activity of TAS-103 against freshly-isolated human colorectal cancer.

[3] Ohyama T, et al. Jpn J Cancer Res. A dual topoisomerase inhibitor, TAS-103, induces apoptosis in human cancer cells.

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Keywords: TAS-103 dihydrochloride, BMS-247615 supplier, Topoisomerase, inhibitors, activators


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