KRN-633
作者：齊岳
發(fā)布時(shí)間：2023-08-23
09:38:00
點(diǎn)擊數(shù)：
產(chǎn)品名稱：KRN-633
產(chǎn)品描述：
| 產(chǎn)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. |
| 靶點(diǎn)活性 | VEGFR1:170 nM, VEGFR3:125 nM, VEGFR2:160 nM |
| 體外活性 | 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). |
| 體內(nèi)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. |
| 激酶實(shí)驗(yàn) | In cell-free kinase assays,with1 μM ATP the IC50 of KRN-633 is from 0.3 nM to 10 μM. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 動物實(shí)驗(yàn) | 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. |
| 別名 | 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 |
存儲
| 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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公司介紹：
西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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