| CAS NO: | 690206-97-4 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 333.74 |
| Cas No. | 690206-97-4 |
| Formula | C16H13ClFN3O2 |
| Solubility | ≥33.4 mg/mL in DMSO; insoluble in H2O; ≥2.85 mg/mL in EtOH with gentle warming |
| Chemical Name | N-(4-chloro-2-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine |
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=C(C=C3)Cl)F)OC |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
ZM 306416是选择性VEGFR抑制剂,IC50值为0.67 μM [1].有报道称ZM 306416抑制EGFR,IC50值小于10 nM [2].
血管内皮生长因子受体(VEGFR)是胞外基质(ECM)的关键分子,与其配体VEGF协作,在血管生成中发挥重要作用.诸多研究证明VEGFRs表达于液体和实体瘤细胞,如NSCLC\黑色素瘤\前列腺癌\白血病\间皮瘤和乳腺癌,并作为临床中有希望的靶点[3].
ZM 306416是高效的VEGFR抑制剂,与其它已报道的VEGFR抑制剂相比具有不同的选择性.用A549-EGFRB细胞进行EGFRB实验表明ZM 306416对VEGFR表现出抑制活性,IC50值为670 nM [1].在人甲状腺滤泡细胞中,ZM 306416处理表现出降低VEGFR2磷酸化\抑制内源性p42/44 MAPK 磷酸化稳态水平的功能[4].
参考文献：
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.
| Description | ZM 306416是VEGFR(Flt和KDR)的抑制剂,对VEGFR1的IC50值为0.33 μM. | |||||
| 靶点 | VEGFR1 | Src | Abl | |||
| IC50 | 0.33 μM | 0.33 μM | 1.3 μM | |||
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