ZM 306416

ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.

Research Areas >> Cancer

KDR:100 nM (IC50)

Flt-1:2 μM (IC50)

ZM-306416 selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 (IC50=0.09±0.007 μM and 0.072±0.001 μM respectively), while sparing the wild type EGFR cell lines A549 and H2030 (IC50>10 μM). ZM-306416 is also found to inhibit the ABL in vitro kinase activity with a less potent IC50 value of 1.3±0.2 μM toward the ABL kinase[2].

[1]. Han SY, Park SS, Lee WG, Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33.

[2]. Antczak C, Mahida JP, Bhinder B, A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99.

Nintedanib (BIBF 1120) | SU5416 | Apatinib Mesylate | PD173074 | Foretinib (GSK1363089) | SU 5402 | Linifanib (ABT-869) | Cediranib | Lucitanib | RAF265 (CHIR-265) | LY2784544 | SU14813 | Dovitinib (TKI-258, CHIR-258) | SAR131675 | Vatalanib (PTK787) 2HCl