ChemicalBook > CAS DataBase List > TAS-115

TAS-115

Product Name: TAS-115
CAS No.: 1190836-34-0
Chemical Name: TAS-115
Synonyms: TAS-115;H2OL3Q4XRD;Pamufetinib;TAS-115,HY-12423;Pamufetinib (TAS-115);TAS-115;TAS 115;TAS115;Pamufetinib, 10 mM in DMSO;4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide;c-Met/HGFR,Inhibitor,TAS 115,TAS115,inhibit,VEGFR,Pamufetinib,Vascular endothelial growth factor receptor;6-Quinolinecarboxamide, 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]phenoxy]-7-methoxy-N-methyl-
CBNumber: CB93175593
Molecular Formula: C27H23FN4O4S
Formula Weight: 518.56
MOL File: 1190836-34-0.mol

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TAS-115 Property

Density: 1.364±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO:10.0(Max Conc. mg/mL);19.28(Max Conc. mM)
pka: 10.07±0.70(Predicted)
form: Solid
color: Off-white to light yellow
InChIKey: ORRNXRYWGDUDOG-UHFFFAOYSA-N
SMILES: N1C2C(=CC(C(NC)=O)=C(OC)C=2)C(OC2=CC=C(NC(NC(CC3=CC=CC=C3)=O)=S)C=C2F)=CC=1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Biorbyt Ltd

Product number: orb573433
Product name: TAS-115
Purity: >98%
Packaging: 100mg
Price: $2541.5
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573433
Product name: TAS-115
Purity: >98%
Packaging: 250mg
Price: $3876
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573433
Product name: TAS-115
Purity: >98%
Packaging: 1g
Price: $5803.8
Updated: 2021/12/16

DC Chemicals

Product number: DC20274
Product name: TAS-115
Purity: >98%
Packaging: 250mg
Price: $2600
Updated: 2021/12/16

DC Chemicals

Product number: DC20274
Product name: TAS-115
Purity: >98%
Packaging: 100mg
Price: $1700
Updated: 2021/12/16

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TAS-115 Chemical Properties,Usage,Production

Uses

Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

in vivo

Pamufetinib (50 mg/kg/d) completely prevents tumor growth during the treatment period. Pamufetinib (200 mg/kg/d) induces a 48% regression from the initial tumor volume in MET-amplified human cancer transplanted models. The estimated 50% effective dose (ED₅₀) of Pamufetinib in this model is 8 mg/kg/d. Pamufetinib significantly prolongs survival of these mice when administered at doses of 50 or 200 mg/kg/d^[1]. Pamufetinib inhibits angiogenesis in PC-9/HGF tumors in vivo. Moreover, the doublet erlotinib and Pamufetinib successfully inhibit PC-9/HGF tumor growth and delay tumor regrowth associated with sustained tumor vasculature inhibition even after cessation of the treatment^[2].

IC 50

VEGFR2: 30 nM (IC₅₀); c-Met: 32 nM (IC₅₀)

References

[1] Fujita H, 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. 2013 Dec;12(12):2685-96. DOI:10.1158/1535-7163.MCT-13-0459
[2] Nakade J, et al. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation. J Thorac Oncol. 2014 Jun;9(6):775-83. DOI:10.1097/JTO.0000000000000170

TAS-115 Preparation Products And Raw materials

Raw materials

Preparation Products

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1190836-34-0, TAS-115Related Search:

TAS-115

TAS-115,HY-12423

TAS-115;TAS 115;TAS115

6-Quinolinecarboxamide, 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]phenoxy]-7-methoxy-N-methyl-

Pamufetinib (TAS-115)

4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide

H2OL3Q4XRD

Pamufetinib

c-Met/HGFR,Inhibitor,TAS 115,TAS115,inhibit,VEGFR,Pamufetinib,Vascular endothelial growth factor receptor

Pamufetinib, 10 mM in DMSO

1190836-34-0

C27H23FN4O4S