Fruquintinib | Potent and selective inhibitor of VEGFR kinase

CAS:
1194506-26-7
Catalog Number:
10-4784
Activity:
Potent and selective inhibitor of VEGFR kinase
Chemical Name:
6-(6,7-Dimethoxyquinazolin-4-yl)oxy-N,2-dimethyl-1-benzofuran-3-carboxamide
Alternate Name:
HMPL-013
Molecular Weight:
393.40
Molecular Formula:
C21H<sub19< sub=””>N3O4</sub19<>
Solubility:
Soluble in DMSO (up to 5 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$215.00

Fruquintinib (1194506-26-7) is a potent and highly selective inhibitor of VEGFR kinase (IC50’s: VEGFR1= 33 nM, VEGFR2 = 35 nM, VEGFR3 = 0.5 nM).1 It potently inhibited VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs and prevented angiogenesis in vitro. Fruquintinib is currently is several clinical trials against metastatic colorectal cancer2 and nonsquamous non-small-cell lung cancer3.

References/Citations:

1) Sun et al. (2014) Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1,2,3 tyrosine kinases for cancer therapy; Cancer Biol. Ther. 15 1635
2) Li et al. (2018) Effect of Fruquintinib vs Placebo on Overall Survival in Patients With Previously Treated Metastatic Colorectal Cancer: The FRESCO Randomized Clinical Trial; JAMA 319 2486
3) Lu et al. (2018) Randomized, Double-Blind, Placebo-Controlled, Multicenter Phase II Study of Fruquintinib After Two Prior Chemotherapy Regimens in Chinese Patients With Advanced Nonsquamous Non-Small-cell Lung Cancer; J. Clin. Oncol. 36 1207

CAS:
1194506-26-7
Catalog Number:
10-4784
Activity:
Potent and selective inhibitor of VEGFR kinase
Chemical Name:
6-(6,7-Dimethoxyquinazolin-4-yl)oxy-N,2-dimethyl-1-benzofuran-3-carboxamide
Alternate Name:
HMPL-013
Molecular Weight:
393.40
Molecular Formula:
C21H<sub19< sub=””>N3O4</sub19<>
Solubility:
Soluble in DMSO (up to 5 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee