ZK-261991

"目录号: HY-15333

Protein Tyrosine Kinase/RTK-

ZK-261991 是一种可口服的VEGF receptor酪氨酸酶抑制剂，能够抑制 VEGFR-2 的活性，IC50值为 5 nM。

VEGFR

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生物活性

Description

ZK-261991 is an orally activeVEGF receptortyrosine kinase inhibitor, withIC50of 5 nM for VEGFR-2.

IC50& Target

IC50: 5 nM (VEGFR-2)[1]

In Vitro

ZK-261991 inhibits cellular receptor autophosphorylation in KDR-PAECs with an IC50of 2 nM. ZK991 inhibits VEGFR-3 autophosphorylation concentration dependently with an IC50of 20 nM[1].

In Vivo

ZK991 results in a significantly reduced recruitment of CD11b+and LYVE-1+cells into the murine cornea. ZK991 significantly improves the graft survival rate after corneal transplantation[1].

References

[1].Deniz Hos, et al. Inflammatory Corneal (Lymph)angiogenesis Is Blocked by VEGFR-Tyrosine Kinase Inhibitor ZK 261991, Resulting in Improved Graft Survival after Corneal Transplantation. Investigative Ophthalmology & Visual Science May 2008, Vol.49, 1836-1842.