|1-(4-((6-氨基-5-((甲氧基亚氨基)甲基)嘧啶-4-基)氧基)-2-氯苯基)-3-乙基脲|CsnPharm

CAS No.: 951151-97-6

JNJ-38158471 Catalog No. CSN26936

JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The vascular endothelial growth factor (VEGF) receptors are important angiogenesis mediators that have been considered as a hallmark of tumor growth and metastasis. JNJ-3815847 is a potent and selective VEGFR-2 inhibitor with an IC50 value of 40nM. It showed no anti-proliferative effects on human cancer cell lines HCT116 and A375 at 100μM. In human umbilical vein endothelial cells (HUVECs), JNJ-38158471 (1 - 500nM) potently inhibited VEGF-dependent auto-phosphorylation of VEGFR-2 in a concentration-dependent manner (90% inhibition at 500nM). JNJ-38158471 treatment (50 - 1000nM) also significantly inhibited VEGF-dependent HUVEC migration. Oral administration of mice with JNJ-38158471 (10 or 100mg/kg/day) for 6 days caused a dose-dependent inhibition of VEGF-dependent blood vessel formation (15% and 83% inhibition, respectively) compared to the vehicle controls. In a mouse A375 melanoma model, treatment with JNJ-38158471 (100mg/kg/day) significantly inhibited tumor growth (90% inhibition) at 28 days of continuous dosing^[1].
参考文献

[1] LaMontagne KR, Butler J, Borowski VB, Fuentes-Pesquera AR, Blevitt JM, Huang S, Li R, Connolly PJ, Greenberger LM. A highly selective, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor has potent activity in vitro and in vivo. Angiogenesis. 2009;12(3):287-96. doi: 10.1007/s10456-009-9151-7

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7413 mL
- 13.7066 mL
- 27.4133 mL
- 5 mM
- 0.5483 mL
- 2.7413 mL
- 5.4827 mL
- 10 mM
- 0.2741 mL
- 1.3707 mL
- 2.7413 mL

技术信息

CAS号

951151-97-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H17ClN6O3

运输

蓝冰

分子量

364.79

别名

溶解度

DMSO	30.0 mg/mL (82.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

JNJ-38158471 Catalog No. CSN26936

靶点选择性

请登录您的专属账户

确认信息