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TAS-120

Chemical Structure : TAS-120

CAS No.: 1448169-71-8

TAS-120 (Futibatinib, TAS120)

Catalog No.: PC-35453Not For Human Use, Lab Use Only.

TAS-120 (Futibatinib, TAS120) is a highly potent, selective, irreversible pan-FGFR inhibitor with IC50 of 0.9 nM for wt FGFR2.

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Biological Activity

TAS-120 (Futibatinib, TAS120) is a highly potent, selective, irreversible pan-FGFR inhibitor with IC50 of 0.9 nM for wt FGFR2.
TAS-120  inhibits cancer cell growth in vitro and shows promising activity in human xenografts of FGFR mutation-bearing tumours.
TAS-120 inhibits mutant and wild-type FGFR2 with similar IC50 (wild-type FGFR2, 0.9 nM; V565I 1.3 nM; N550H, 3.6 nM; E566G, 2.4 nM) and has shown efficacy in FGFR inhibitor-resistant cell lines.

Physicochemical Properties

M.Wt 418.457
Formula C22H22N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en1-one

References

1. Hiroaki Ochiiwa, et al. Abstract A270: TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. AACR 2013.

2. Kalyukina M, et al. ChemMedChem. 2019 Jan 2. doi: 10.1002/cmdc.201800719.

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