Pamufetinib
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 98.28%
- CAS No.: 1190836-34-0
- Formula: C27H23FN4O4S
- Molecular Weight:518.56
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
HY-12050
CP-673451PDGFR Inhibitor -
HY-13016
CabozantinibVEGFR2/MET Inhibitor -
HY-10338
ForetinibMET/VEGFR2/KDR Inhibitor -
HY-12423A
Pamufetinib mesylateVEGFR/c-Met/HGFR Inhibitor -
HY-10981
LenvatinibVEGFR/FGFR Inhibitor -
HY-18696
AMG-337MET Kinase Inhibitor -
HY-10065
AxitinibTyrosine Kinase Inhibitor -
HY-16590
X-376ALK and MET Inhibitor -
HY-13016R
Cabozantinib (Standard)VEGFR2/MET Inhibitor -
HY-10991
MGCD-265 analogc-Met/VEGFR2 Inhibitor -
HY-111787
Elzovantinibc-Met/HGFR Inhibitor
All VEGFR Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
VEGFR2 30 nM (IC50) |
c-Met 32 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | GI50 |
>10 μM
Compound: TAS-115
|
Cytotoxicity against HUVEC assessed as inhibition of VEGF-independent growth after 72 hrs by CellTiter-Glo method
Cytotoxicity against HUVEC assessed as inhibition of VEGF-independent growth after 72 hrs by CellTiter-Glo method
|
[PMID: 26717201] |
In Vitro
Pamufetinib is ATP antagonism with inhibition constant (Ki) values against rVEGFR2 and rMET of 12 and 39 nM, respectively. Pamufetinib inhibits the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. Pamufetinib induces less damage in various normal cells than do other VEGFR inhibitors[1]. Pamufetinib does not affect the growth of PC-9 or HCC827 cells at concentrations less than 10 μM; however, the combined use of Pamufetinib with erlotinib reverses HGF-induced resistance in the cell lines in a concentration-dependent manner. Pamufetinib inhibits VEGF production by cancer cells and endothelial proliferation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1190836-34-0
-
Appearance Solid
-
Molecular Weight 518.56
-
Formula C27H23FN4O4S
-
Color Off-white to light yellow
-
SMILES
O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3F)C2=C1)NC
-
Synonyms
TAS-115
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (48.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (282 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9284 mL | 9.6421 mL | 19.2842 mL | 48.2104 mL |
| 5 mM | 0.3857 mL | 1.9284 mL | 3.8568 mL | 9.6421 mL | |
| 10 mM | 0.1928 mL | 0.9642 mL | 1.9284 mL | 4.8210 mL | |
| 15 mM | 0.1286 mL | 0.6428 mL | 1.2856 mL | 3.2140 mL | |
| 20 mM | 0.0964 mL | 0.4821 mL | 0.9642 mL | 2.4105 mL | |
| 25 mM | 0.0771 mL | 0.3857 mL | 0.7714 mL | 1.9284 mL | |
| 30 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6070 mL | |
| 40 mM | 0.0482 mL | 0.2411 mL | 0.4821 mL | 1.2053 mL |
Pamufetinib Related Classifications
HY-12423 Related Classifications
Powered by Bioz