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Fruquintinib

Chemical Structure : Fruquintinib

CAS No.: 1194506-26-7

Fruquintinib (HMPL-013, HMPL013)

Catalog No.: PC-45746Not For Human Use, Lab Use Only.

Fruquintinib (HMPL-013) is a potent and highly selective small molecule inhibitor of VEGFR1/2/3 with IC50 of 33/3/5/0.5 nM, respectively.

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Biological Activity

Fruquintinib (HMPL-013) is a potent and highly selective small molecule inhibitor of VEGFR1/2/3 with IC50 of 33/3/5/0.5 nM, respectively.
Fruquintinib (HMPL-013) weakly inhibits RET, FGFR-1 and c-kit kinases.
Fruquintinib (HMPL-013) demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC50 of 0.6 nM and 1.7 nM, respectively.
Fruquintinib (HMPL-013) suppresses tumor growth inhibition in a panel of tumor xenograft and patient derive xenograft models in mouse.
Fruquintinib (HMPL-013) is orally active.

Physicochemical Properties

M.Wt 393.3927
Formula C21H19N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 7.75 mg/mL

Chemical Name/SMILES

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

References

1. Sun Q, et al. Cancer Biol Ther. 2014;15(12):1635-45.

2. Gu Y, et al. Cancer Chemother Pharmacol. 2014 Jul;74(1):95-115.

3. Cao J, et al. Cancer Chemother Pharmacol. 2016 Aug;78(2):259-69.

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