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YM-359445

Chemical Structure : YM-359445

CAS No.: 1020067-28-0

YM-359445 (YM359445)

Catalog No.: PC-61439Not For Human Use, Lab Use Only.

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM); inhibits VEGFR2 tyrosine kinase activity completely at 0.03 uM, inhibits HUVEC proliferation induced by VEGF with IC50 of 1.5 nM; inhibits VEGF-stimulated autophosphorylation of VEGFR2 at 0.1 nM, also inhibits sprout formation of endothelial cells at 3 nM; not only inhibits tumor growth but also reduces its vasculature in mice bearing various tumors, including paclitaxel-resistant tumors.

Physicochemical Properties

M.Wt 662.718
Formula C32H34N6O8S
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

(3Z)-3-[6-[(4-methylpiperazin-1-yl)methyl]quinolin-2(1H)-ylidene]-2-oxoindoline-6-carbaldehyde O-(1,3-thiazol-4-ylmethyl)oxime mono-l-tartrate

References

1. Amino N, et al. Clin Cancer Res. 2006 Mar 1;12(5):1630-8.

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