KRN-633
作者：齐岳
发布时间：2023-08-23
09:38:00
点击数：
产品名称：KRN-633
产品描述：
| 产品描述 | KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively. |
| 靶点活性 | VEGFR1:170 nM, VEGFR3:125 nM, VEGFR2:160 nM |
| 体外活性 | In human umbilical vein endothelial cells, KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β with IC50 of 11.7, 1.16, 8.01, 130 nM, respectively. In endothelial cells, KRN-633 inhibits the formation of the capillary tube. KRN-633 suppress the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). |
| 体内活性 | In athymic mouse and rat xenograft models, KRN-633 was able to inhibit tumor growth in various tissue sources such as lungs, colon, and prostate. It was also observed that in the non-necrosis region of tumor grafts, the number of endothelial cells was reduced and vascular permeability decreased. In the regenerated tumors, KRN-633 can also ablate tumor growth. |
| 激酶实验 | In cell-free kinase assays,with1 μM ATP the IC50 of KRN-633 is from 0.3 nM to 10 μM. |
| 细胞实验 | Cancer cells, such as A549, Ls174T, HT29, DU145, LNCap, and PC-3 cells, are cultured for 24 hours, then add KRN-633 (0.01 to 10 μM)that is prepared in 0.1% DMSO in the medium growing for 96 hours. |
| 动物实验 | In tumor xenografts mice model, are treated with KRN-633(10-100 mg/kg) once or twice per day. In human tumor xenografts athymic rats (BALB/cA, Jcl-nu), when the tumors reach the average size indicated (162 to 657 mm3), and are treated with KRN-633 either once or twice per day. After 14days treatment, Calculate the tumor growth inhibition. |
| 别名 | N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲, KRN633 |
| 分子量 | 416.86 |
| 分子式 | C20H21ClN4O4 |
| CAS No. | 286370-15-8 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 8 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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