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ZM 306416

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Chemical Structure| 690206-97-4 同义名 : CB 676475
CAS号 : 690206-97-4
货号 : A331607
分子式 : C16H13ClFN3O2
纯度 : 99%+
分子量 : 333.745
MDL号 : MFCD02683969
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(149.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • VEGFR1

    VEGFR1, IC50:0.33 μM
描述 ZM-306416, a vascular endothelial growth factor receptor (VEGFR) antagonist, was identified as a potent inhibitor of EGFR function[3]. The VEGFR1/2 inhibitors, ZM306416 and KRN633, lead to a dose-dependent decrease in mineralization[4]. ZM-306416 induced 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[3]. Ki8751, a selective VEGFR2 inhibitor, completely suppressed the effect of VEGF121 on SCE cell permeability, although ZM306416, a selective VEGFR1 inhibitor, did not affect the VEGF121-induced decrease in TEER (transendothelial electrical resistance)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

14.98mL

3.00mL

1.50mL

29.96mL

5.99mL

3.00mL
参考文献

[1]Antczak C, Mahida JP, et al. 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.

[2]Wilkinson J, Hallis T, et al. Development and validation of a cell-based assay for the nuclear receptor retinoid-related orphan receptor gamma. Assay Drug Dev Technol. 2011 Apr;9(2):125-35.

[3]Antczak C, Mahida JP, Bhinder B, Calder PA, Djaballah H. 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

[4]McLaughlin KI, Milne TJ, Zafar S, Zanicotti DG, Cullinan MP, Seymour GJ, Coates DE. The in vitro effect of VEGF receptor inhibition on primary alveolar osteoblast nodule formation. Aust Dent J. 2020 Sep;65(3):196-204

[5]Fujimoto T, Inoue T, Maki K, Inoue-Mochita M, Tanihara H. Vascular Endothelial Growth Factor-A Increases the Aqueous Humor Outflow Facility. PLoS One. 2016 Sep 1;11(9):e0161332