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KRN-633 是一种 VEGFR 抑制剂,能够一种 VEGFR1 (IC50:170 nM)、VEGFR2 (IC50:160 nM)、VEGFR3 (IC50:125 nM)。
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KRN-633 是一种 VEGFR 抑制剂,能够一种 VEGFR1 (IC50:170 nM)、VEGFR2 (IC50:160 nM)、VEGFR3 (IC50:125 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 237 | 现货 | |
5 mg | ¥ 573 | 现货 | |
10 mg | ¥ 978 | 现货 | |
25 mg | ¥ 1,670 | 现货 | |
50 mg | ¥ 2,490 | 现货 | |
100 mg | ¥ 3,550 | 现货 | |
200 mg | ¥ 4,870 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 598 | 现货 |
产品描述 | KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633(KRN633) for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively. |
靶点活性 | VEGFR2:160 nM, VEGFR3:125 nM, VEGFR1:170 nM |
体外活性 | 在人类脐静脉内皮细胞中,KRN-633能够抑制VEGFR-1、VEGFR2、c-Kit及PDGFR-β的酪氨酸磷酸化作用,其半抑制浓度(IC50)分别为11.7、1.16、8.01、130 nM。在内皮细胞中,KRN-633抑制毛细血管管腔的形成,并能够抑制VEGF驱动的HUVEC增殖(IC50=14.9 nM)。 |
体内活性 | 在裸鼠和大鼠异种移植模型中,KRN-633能够抑制来自多种组织源的肿瘤生长,包括肺、结肠和前列腺等。同时观察到,在肿瘤移植物的非坏死区域,内皮细胞数量减少,血管通透性降低。在再生的肿瘤中,KRN-633同样能够消灭肿瘤生长。 |
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 |
Smiles | CCCNC(=O)Nc1ccc(Oc2ncnc3cc(OC)c(OC)cc23)cc1Cl |
密度 | 1.321 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 6 mg/mL (14.39 mM) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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