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ZM 306416
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ZM 306416图片
CAS NO:690206-97-4
包装与价格：
包装价格(元)
10mg电议
50mg电议
500mg电议
1g电议

产品介绍
ZM-306416 (CB 676475) 是一种有效的 VEGFR 抑制剂，对 KDR 和 Flt 的 IC50 分别为 0.1 和 2 μM。 ZM-306416 也是一种 EGFR 抑制剂，IC50<10 nM。
Cas No.690206-97-4
别名CB 676475
化学名N-(4-chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine
Canonical SMILESCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC
分子式C16H13ClFN3O2
分子量333.74
溶解度≥ 33.4mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ZM 306416 is a selective inhibitor of VEGFR with IC50 value of 0.67μM [1]. It is also reported that ZM 306416 inhibits EGFR with IC50 value less than 10 nM [2].

Vascular endothelial growth factor receptor (VEGFR) is a key element of the extracellular matrix(ECM) and plays an important role in angiogenesis cooperating with its ligand VEGF. Several studies have demonstrated that VEGFRs expressed in liquid and solid tumor cells, such as NSCLC, melanoma, prostate cancer, leukemia, mesothelioma, and breast cancer and are being regarded as a promising target in clinical [3].

ZM 306416 is a potent VEGFR inhibitor and has a different selectivity with other reported VEGFR inhibitors. Using A549-EGFRB cells for EGFRB assay revealed that ZM 306416 exhibited inhibitory activity on VEGFR with IC50 value of 670 nM [1]. When tested with human thyroid follicular cells, ZM 306416 treatment exhibited function on reducing VEGFR2 phosphorylation and inhibiting endogenous, steady-state levels of p42/44 MAPK phosphorylation [4].

References:
1.  Antczak, C., 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. 17(7): p. 885-99.
2.  Choi KJ, Baik IH, Ye SK et al. Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull. 2015;38(7):986-91.
3.  Choi, K.J., et al., Molecular Targeted Therapy for Hepatocellular Carcinoma: Present Status and Future Directions. Biol Pharm Bull, 2015. 38(7): p. 986-91.
4.  Susarla, R., J.C. Watkinson, and M.C. Eggo, Regulation of human thyroid follicular cell function by inhibition of vascular endothelial growth factor receptor signalling. Mol Cell Endocrinol, 2012. 351(2): p. 199-207.