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
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
N-Bromosuccinimide Price
- Product number
- orb573433
- Product name
- TAS-115
- Purity
- >98%
- Packaging
- 100mg
- Price
- $2541.5
- Updated
- 2021/12/16
- Product number
- orb573433
- Product name
- TAS-115
- Purity
- >98%
- Packaging
- 250mg
- Price
- $3876
- Updated
- 2021/12/16
- Product number
- orb573433
- Product name
- TAS-115
- Purity
- >98%
- Packaging
- 1g
- Price
- $5803.8
- Updated
- 2021/12/16
- Product number
- DC20274
- Product name
- TAS-115
- Purity
- >98%
- Packaging
- 100mg
- Price
- $1700
- Updated
- 2021/12/16
- Product number
- DC20274
- Product name
- TAS-115
- Purity
- >98%
- Packaging
- 250mg
- Price
- $2600
- Updated
- 2021/12/16
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
TAS-115 Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
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- 32435
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- 708-557-7486
- sales@invivochem.cn
- Country
- United States
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- +1-781-999-5354;
- support@targetmol.com
- Country
- United States
- ProdList
- 39035
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- Tel
- tp@aladdinsci.com
- Country
- United States
- ProdList
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- Advantage
- 58