TAS120 free base · Synonyms: Futibatinib

TAS120 is an orally bioavailable, highly selective, and irreversible FGFR inhibitor.

For research use only. Not for human or veterinary use.

Target FGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

TAS120 structure

CAS No.: 1448169-71-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 465.00	BP-01892-500mg	In stock	Get quote
1 g	USD 685.00	BP-01892-1g	In stock	Get quote
2 g	USD 1,185.00	BP-01892-2g	In stock	Get quote
5 g	Inquire	BP-01892-5g	Inquire	Inquire
10 g	Inquire	BP-01892-10g	Inquire	Inquire

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Description

TAS120 is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively.

Biological activity

In Vitro Futibatinib (TAS-120) covalently binds to a highly conserved P-loop cysteine residue in the ATP pocket of FGFR. In Vivo Futibatinib (TAS-120) (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. Futibatinib (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.

Identifiers

SMILES: COC1=CC(=CC(OC)=C1)C#CC1=NN([C@H]2CCN(C2)C(=O)C=C)C2=NC=NC(N)=C12
InChIKey: KEIPNCCJPRMIAX-HNNXBMFYSA-N

Specifications

MW (average): 418.4485
Formula: C₂₂H₂₂N₆O₃
CAS No.: 1448169-71-8
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : >25 mg/mL (69.30 mM)

Documents

References

[1]. Goyal L, et al. TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma. Cancer Discov. 2019 Aug;9(8):1064-1079.

[2]. Kalyukina M, et al. TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure. ChemMedChem. 2019 Feb 19;14(4):494-500.

[3]. Lamarca A, et al. Molecular targeted therapies: Ready for "prime time" in biliary tract cancer [published online ahead of print, 2020 Mar 12]. J Hepatol. 2020;S0168-8278(20)30165-3.

Same target

Search FGFR

Same research area

Search Cancer