Fruquintinib , 10mMinDMSO , 1194506-26-7

CAS NO.：1194506-26-7

Empirical Formula: C21H19N3O5

Molecular Weight: 393.39

MDL number: MFCD28502149

PRODUCT Properties

• Boiling point: 600.5±55.0 °C(Predicted)
• Density: 1.302±0.06 g/cm3(Predicted)
• storage temp.: Sealed in dry,Store in freezer, under -20°C
• solubility: Soluble in DMSO (up to 5 mg/ml).
• pka: 14.35±0.46(Predicted)
• form: solid
• color: White
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
• InChI: InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
• InChIKey: BALLNEJQLSTPIO-UHFFFAOYSA-N
• SMILES: O1C2=CC(OC3=C4C(=NC=N3)C=C(OC)C(OC)=C4)=CC=C2C(C(NC)=O)=C1C

Description and Uses

Fruquintinib is a VEGFR inhibitor (IC₅₀s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively). It also inhibits RET, FGFR1, and c-Kit (IC₅₀s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases. Fruquintinib inhibits VEGF-A-induced proliferation of human umbilical vein endothelial cells (HUVECs) and VEGF-C-induced proliferation of human lymphatic endothelial cells (HLECs; IC₅₀s = 1.7 and 4.2 nM, respectively). It decreases tube formation by HUVECs by 74 and 94% when used at concentrations of 30 and 300 nM, respectively. Fruquintinib (0.5-20 mg/kg per day for 21 days) reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models.

Fruquintinib is a multi-targeted tyrosine kinase inhibitor, a third-line regimen involved in the treatment of advanced non-small cell lung cancer in humans. Fruquintinib is a potent, highly selective and orally active inhibitor of VEGFR1, 2, 3 tyrosine kinases.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338