CAS 1194506-26-7|Fruquintinib

Introduction：Basic information about CAS 1194506-26-7|Fruquintinib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Fruquintinib BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Fruquintinib
CAS Number	1194506-26-7	Molecular Weight	393.393
Density	1.3±0.1 g/cm3	Boiling Point	600.5±55.0 °C at 760 mmHg
Molecular Formula	C₂₁H₁₉N₃O₅	Melting Point	/
MSDS	/	Flash Point	317.0±31.5 °C

Names

Name	6-(6,7-dimethoxyquinazolin-4-yloxy)-N,2-dimethylbenzofuran-3-carboxamide
Synonym	More Synonyms

Fruquintinib BiologicalActivity

Description	Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.
Related Catalog	Research Areas >>Cancer
Target	VEGFR1:33 nM (IC50) VEGFR2:35 nM (IC50) VEGFR3:0.5 nM (IC50)
In Vitro	Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC50s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours[1].
In Vivo	Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4∼98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg[1].
Cell Assay	Primary HUVECs or HLECs in exponential phase are suspended in 100 μL of RPMI-1640 media containing 0.5% FBS, and seeded at 5000 cell/well in 96-well plates pre-coated with 0.2% gelatin or fibronectin, and incubated overnight in a 5% CO2, 37°C incubator. Fruquintinib and VEGF-A165 or VEGF-C (50 ng/mL) are added and incubated for 48 hours. Viability of the cells is determined using CCK-8 assay format[1].
Animal Admin	Mice: The patient derived xenograft models are established after the primary tumor adopted serial passages in vivo. Once tumors have grown to 100-300 mm3, the animals are randomly assigned with 6-8 animals per group. The mice are treated orally with the vehicle (control group) or fruquintinib at a dose range of 0.5-20 mg/kg suspended in the vehicle (treated group) once daily for 3 weeks. In combination studies, docetaxel (Taxotere, 5 mg/kg) or oxaliplatin (10 mg/kg) is administered to nude mouse via intravenous injection, once a week. Tumor size and body weights are measured 3 times a week. Tumor volumes (TV) are calculated[1].
References	[1]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	600.5±55.0 °C at 760 mmHg
Molecular Formula	C₂₁H₁₉N₃O₅
Molecular Weight	393.393
Flash Point	317.0±31.5 °C
Exact Mass	393.132477
PSA	95.71000
LogP	3.08
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.639
Storage condition	-20°C

Synonyms

3-Benzofurancarboxamide, 6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-

6-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N,2-dimethyl-1-benzofuran-3-carboxamide

6-[(6,7-dimethoxy-4-quinazolinyl)oxy]-2-methyl-benzofuran-3-carboxamide

HMPL-013

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