Futibatinib (TAS-120)

Catalog No.S8848 Batch:S884802

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Technical Data

Formula

C22H22N6O3

Molecular Weight 418.45 CAS No. 1448169-71-8
Solubility (25°C)* In vitro DMSO 84 mg/mL (200.74 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Targets
FGFR2 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
1.4 nM 1.6 nM 1.8 nM 3.7 nM
In vitro

Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

Protocol (from reference)

Animal Study:

[2]

  • Animal Models

    Nude mice

  • Dosages

    0.15, 0.5, 1.5, & 5 mg/kg

  • Administration

    p.o.

Selleck's Futibatinib (TAS-120) has been cited by 16 publications

FGFR inhibition blocks NF-ĸB-dependent glucose metabolism and confers metabolic vulnerabilities in cholangiocarcinoma [ Nat Commun, 2024, 15(1):3805] PubMed: 38714664
Understanding and Overcoming Resistance to Selective FGFR inhibitors Across FGFR2-Driven Malignancies [ Clin Cancer Res, 2024, 10.1158/1078-0432.CCR-24-1834] PubMed: 39226398
iPSC-derived megakaryocytes and platelets accelerate wound healing and angiogenesis [ Stem Cell Res Ther, 2024, 15(1):364] PubMed: 39402677
Paradoxical cancer cell proliferation after FGFR inhibition through decreased p21 signaling in FGFR1-amplified breast cancer cells [ Breast Cancer Res, 2024, 26(1):54] PubMed: 38553760
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer [ Cancer Discov, 2023, 13(9):1998-2011] PubMed: 37377403
Dietary phosphorus consumption alters T cell populations, cytokine production, and bone volume in mice [ JCI Insight, 2023, 8(10)e154729] PubMed: 37079375
Unraveling the Mechanisms of Sensitivity to Anti-FGF Therapies in Imatinib-Resistant Gastrointestinal Stromal Tumors (GIST) Lacking Secondary KIT Mutations [ Cancers (Basel), 2023, 15(22)5354] PubMed: 38001614
EGFR Inhibition Potentiates FGFR Inhibitor Therapy and Overcomes Resistance in FGFR2 Fusion-Positive Cholangiocarcinoma [ Cancer Discov, 2022, 12(5):1378-1395] PubMed: 35420673

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.