A multi-kinase inhibitor
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TAS 115 (methanesulfonate)

Item No. 33593

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide, monomethanesulfonate
CAS Number
1688673-09-7
Molecular Formula
C27H23FN4O4S • CH4O3S
Formula Weight
614.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: slightly solublePBS (pH 7.2): slightly solubleWater: slightly soluble
λmax
244 nm
SMILES
O=C(C1=CC2=C(OC3=CC=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3F)C=CN=C2C=C1OC)NC.O=S(O)(C)=O
InChi Code
InChI=1S/C27H23FN4O4S.CH4O3S/c1-29-26(34)19-14-18-21(15-24(19)35-2)30-11-10-22(18)36-23-9-8-17(13-20(23)28)31-27(37)32-25(33)12-16-6-4-3-5-7-16;1-5(2,3)4/h3-11,13-15H,12H2,1-2H3,(H,29,34)(H2,31,32,33,37);1H3,(H,2,3,4)
InChi Key
NUYQWFCUOAVQAL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    TAS 115 is a multi-kinase inhibitor that inhibits the growth factor receptors PDGFRα and PDGFRβ (IC50s = 0.81 and 7.06 nM, respectively), c-FMS (IC50 = 15 nM), VEGFR2 and VEGFR1 (IC50s = 30 and 140 nM, respectively), Met (IC50 = 32 nM), and FGFR2 (IC50 = 340 nM).1,2 It also inhibits Axl, c-Kit, Src, and FLT1.1 TAS 115 inhibits VEGF-induced VEGFR2 phosphorylation in human umbilical vein endothelial cells (HUVECs) and Met phosphorylation in Met-amplified MKN45 human gastric cancer cells. It also inhibits VEGF-dependent, but not VEGF-independent, growth of HUVECs (IC50s = 0.019 and 19.3 µM, respectively) and of Met-amplified MKN45, but not Met-inactivated, human MCF-7 breast cancer cells (GI50s = 0.032 and >10 µM, respectively). TAS 115 reduces tumor growth in a MKN45 mouse xenograft model (ED50 = 8 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fujita, H., Miyadera, K., Kato, M., et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol. Cancer Ther. 12(12), 2685-2696 (2013).

    2. Koyama, K., Goto, H., Morizumi, S., et al. The tyrosine kinase inhibitor TAS-115 attenuates bleomycin-induced lung fibrosis in mice. Am. J. Respir. Cell Mol. Biol. 60(4), 478-487 (2019).