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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 205  USD205 In stock
25mg USD 400  USD400 In stock
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Quality Control
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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 418.45
Formula C22H22N6O3
CAS Number 1448169-71-8
Purity 99.94%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
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

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