"目錄號: HY-13785

Protein Tyrosine Kinase/RTK-

ZM-306416(CB 676475)是VEGFR選擇性抑制劑（IC50為670nM），對于Flk-1(KDR)和Flt的IC50分別為100nM和2μM。

Bcr-AblSrcVEGFR

相關(guān)產(chǎn)品

Sorafenib-Dasatinib-Nocodazole-BIBF 1120-SU5416-Regorafenib-Ponatinib-Sunitinib-Cabozantinib-Nilotinib-Imatinib Mesylate-Vandetanib-Lenvatinib-Saracatinib-Apatinib-

生物活性

Description

ZM-306416(CB 676475) is a VEGFR inhibitor that inhibits Flk-1 (KDR) (IC50=100 nM) and Flt (IC50 =2 μM); displays 4-fold selectivity over FGFR-1; inhibitor of c-Abl, Flt-1 and Src.IC50 Value: 0.67uM(VEGFR); 0.33±0.08uM(Src); 1.3±0.2 μM(Abl)Target: VEGFR; Src; Ablin vitro: 306416 was found to be very potent toward the EGFR kinase with an IC50 value lower than 10 nM, reaching our assay detection limit and confirming our result using the EGFRB assay. ZM-306416 exhibited inhibitory activity across all three kinases of the panel, yielding IC50 values of 0.33±0.08 μM for SRC, 0.33±0.04 μM for VEGFR1, and 1.3±0.2 μM for ABL kinases [1].

References

[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.