Shopping Cart
- Remove All
- Your shopping cart is currently empty
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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $123 | In Stock | |
10 mg | $179 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $538 | In Stock | |
100 mg | $697 | In Stock | |
200 mg | $989 | In Stock | |
1 mL x 10 mM (in DMSO) | $136 | In Stock |
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] |
Alias | TAS120, FGFR-IN-1 |
Molecular Weight | 418.45 |
Formula | C22H22N6O3 |
Cas No. | 1448169-71-8 |
Smiles | COc1cc(OC)cc(c1)C#Cc1nn([C@H]2CCN(C2)C(=O)C=C)c2ncnc(N)c12 |
Relative Density. | 1.33 g/cm3 (Predicted) |
Storage | Powder: -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
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.