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Futibatinib

🥰Excellent
Catalog No. T5044Cas No. 1448169-71-8
Alias TAS120, FGFR-IN-1

Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]

Futibatinib

Futibatinib

🥰Excellent
Purity: 99.14%
Catalog No. T5044Alias TAS120, FGFR-IN-1Cas No. 1448169-71-8
Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]
Pack SizePriceAvailabilityQuantity
1 mg$48In Stock
5 mg$123In Stock
10 mg$179In Stock
25 mg$347In Stock
50 mg$538In Stock
100 mg$697In Stock
200 mg$989In Stock
1 mL x 10 mM (in DMSO)$136In Stock
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Purity:99.14%
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Product Introduction

Bioactivity
Description
Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]
Targets&IC50
FGFR2:1.3 nM (IC50), FGFR1:3.9 nM (IC50), FGFR2 (V5651):1-3 nM (IC50), FGFR2 (WT):0.3 nM (IC50), FGFR3:1.6 nM (IC50), FGFR4:8.3 nM (IC50), FGFR2 (N550H):3.6 nM (IC50), FGFR2 (E566G):2.4 nM (IC50)
In vitro
TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. TAS-120 shows anti-tumor effect by administering at moderate intervals, such as intermittent administration of every other day dosing and 2 times/week, and reducing the sustained elevation and weight suppression blood phosphorus level, and take a antitumor effective as daily administration.
In vivo
METHODS: Patient-derived ICC xenograft (PDX) model mice were treated with 25 mg/kg Futibatinib(TAS-120) orally daily for 3 and 14 days prior to harvest. Tumor samples were collected for biochemical analysis and histological processing.
RESULTS Treatment of MG69 PDX tumors with TAS-120 (beginning when they reached ~500 mm in volume 3) resulted in tumor regression and complete proliferation arrest, with effects evident within three days and sustained over the 14-day treatment course. [1]
AliasTAS120, FGFR-IN-1
Chemical Properties
Molecular Weight418.45
FormulaC22H22N6O3
Cas No.1448169-71-8
SmilesCOc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12
Relative Density.1.33 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (119.49 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3898 mL11.9489 mL23.8977 mL119.4886 mL
5 mM0.4780 mL2.3898 mL4.7795 mL23.8977 mL
10 mM0.2390 mL1.1949 mL2.3898 mL11.9489 mL
20 mM0.1195 mL0.5974 mL1.1949 mL5.9744 mL
50 mM0.0478 mL0.2390 mL0.4780 mL2.3898 mL
100 mM0.0239 mL0.1195 mL0.2390 mL1.1949 mL

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