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Tipiracil

Cat. No. M13558
Tipiracil Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 150  USD150 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.

Chemical Information
Molecular Weight 242.66
CAS Number 183204-74-2
Form Solid
Solubility (25°C) Water 1 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] Ioannis A Voutsadakis. J Clin Med. Biomarkers of Trifluridine-Tipiracil Efficacy

[2] Akihito Kawazoe, et al. Lancet Gastroenterol Hepatol. Safety and activity of trifluridine/tipiracil and ramucirumab in previously treated advanced gastric cancer: an open-label, single-arm, phase 2 trial

[3] Akihito Kawazoe, et al. Expert Rev Gastroenterol Hepatol. Trifluridine/tipiracil for the treatment of metastatic gastric cancer

[4] Connie Kang, et al. Drugs. Trifluridine/Tipiracil: A Review in Metastatic Gastric Cancer

[5] Kohei Shitara, et al. Lancet Oncol. Trifluridine/tipiracil versus placebo in patients with heavily pretreated metastatic gastric cancer (TAGS): a randomised, double-blind, placebo-controlled, phase 3 trial

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