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PAN-90806

Chemical Structure : PAN-90806

CAS No.: 252003-65-9

PAN-90806 (CP-547632;CP547632)

Catalog No.: PC-61438Not For Human Use, Lab Use Only.

PAN-90806 (CP-547632, CP547632) is a highly potent, ATP-competitive, orally active VEGFR-2 inhibitor that blocks VEGFR-2 kinase autophosphorylation (IC50=11 nM) and VEGF-induced VEGFR-2 phosphorylation (IC50=5 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PAN-90806 (CP-547632, CP547632) is a highly potent, ATP-competitive, orally active VEGFR-2 inhibitor that blocks VEGFR-2 kinase autophosphorylation (IC50=11 nM) and VEGF-induced VEGFR-2 phosphorylation (IC50=5 nM); is approximately equipotent (<10-fold) against VEGFR-2, bFGF receptor and EGFR/Tie-2 chimera, 250-1000-fold selectivity over PDGFRβ, EGFR and InsR; inhibits tumor-associated VEGFR-2 phosphorylation with decreased microvascular density and significant tumor growth inhibition in a number of tumor models.

Other Indication

Phase 1 Clinical

Physicochemical Properties

M.Wt 532.4
Formula C20H24BrF2N5O3S
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

3-((4-bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxamide

References

1. Beebe JS, et al. Cancer Res. 2003 Nov 1;63(21):7301-9.

2. Cohen RB, et al. Cancer Chemother Pharmacol. 2007 Jun;60(1):81-9.

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