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Futibatinib (TAS-120)

Cat. No. M10026
Futibatinib (TAS-120) Structure
Synonym:

TAS-120

Size Price Availability Quantity
2mg USD 90  USD90 In stock
5mg USD 140  USD140 In stock
10mg USD 210  USD210 In stock
25mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Futibatinib (TAS-120) is an oral bioavailable, highly selective and irreversible FGFR inhibitor with IC50 of 3.9, 1.3, 1.6 and 8.3 nM against the four FGFR 1-4 subtypes, respectively. Futibatinib inhibited mutant and wild-type FGFR2 with IC50 similarity (wild-type FGFR2=0.9 nM; V5651 = 1 to 3 nM; N550H = 3.6 nM. E566G = 2.4 nM).

Chemical Information
Molecular Weight 418.45
Formula C22H22N6O3
CAS Number 1448169-71-8
Solubility (25°C) DMSO ≥ 60 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] Hiroshi Sootome, et al. Cancer Res. Futibatinib Is a Novel Irreversible FGFR 1-4 Inhibitor That Shows Selective Antitumor Activity against FGFR-Deregulated Tumors

[2] R Bahleda, et al. Ann Oncol. Phase I, first-in-hυmαn study of futibatinib, a highly selective, irreversible FGFR1-4 inhibitor in ραtιents with advanced solid tumors

[3] Robert Roskoski Jr. Pharmacol Res. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder

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Keywords: Futibatinib (TAS-120), TAS-120 supplier, FGFR, inhibitors, activators


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