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PF-00337210

Chemical Structure : PF-00337210

CAS No.: 854514-88-8

PF-00337210 (PF 00337210;PF00337210;PF-210;PF-337210)

Catalog No.: PC-60958Not For Human Use, Lab Use Only.

A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively; inhibits the autophosphorylation of human and murine VEGFR-2 with IC50 of 0.87 nM and 0.83 nM, respectively; is less potent against KIT (9.6 nM), CSF1-R (13 nM), PDGFR-α (11 nM) and PDGFR-β (29 nM), and does not inhibit Flt-3 (>10 uM); shows dose-dependent anti-tumor efficacy in preclinical tumor models.

Solid Tumors

Phase 1 Clinical

Physicochemical Properties

M.Wt 461.518
Formula C26H27N3O5
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

10 mM in DMSO

Chemical Name/SMILES

N,2-dimethyl-6-[7-(2-morpholin-4-ylethoxy)quinolin-4-yl]oxy-1-benzofuran-3-carboxamide

References

1. Bruce JY, et al. Cancer Chemother Pharmacol. 2016 Mar;77(3):527-38.

2. Tami Marrone, et al. AACR Annual Meeting-- Apr 14-18, 2007; Los Angeles, CA

3. Majeti BK, et al. BMC Cancer. 2013 Apr 29;13:213.

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