An orally bioavailable, irreversible inhibitor of FGFRs
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TAS 120

Item No. 21136

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one
CAS Number
1448169-71-8
Molecular Formula
C22H22N6O3
Formula Weight
418.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 1 mg/mlEthanol: 1 mg/ml
λmax
210, 301 nm
SMILES
COC1=CC(OC)=CC(C#CC2=NN([C@H]3CCN(C(C=C)=O)C3)C4=NC=NC(N)=C42)=C1
InChi Code
InChI=1S/C22H22N6O3/c1-4-19(29)27-8-7-15(12-27)28-22-20(21(23)24-13-25-22)18(26-28)6-5-14-9-16(30-2)11-17(10-14)31-3/h4,9-11,13,15H,1,7-8,12H2,2-3H3,(H2,23,24,25)/t15-/m0/s1
InChi Key
KEIPNCCJPRMIAX-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $63

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    TAS 120 is an orally bioavailable inhibitor of fibroblast growth factor receptors (FGFRs) that irreversibly inhibits all four FGFR subtypes at nanomolar concentrations.1 It prevents phosphorylation of FGFRs and impedes downstream signaling pathways in cells.1 TAS 120 blocks the proliferation of human cancer cell lines with FGFR gene abnormalities but does not alter the growth of cell lines with wild-type FGFR.1 It inhibits FGFR phosphorylation in tumors and tumor growth in human xenograft mouse models in a dose-dependent manner.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ochiiwa, H., Fujita, H., Itoh, K., et al. Abstract A270: TAS-120, a highly potent andselective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. Mol. Cancer Ther. 12(11), (2013).