产品说明书

JNJ-38158471

Print
Chemical Structure| 951151-97-6 同义名 : CS-2660
CAS号 : 951151-97-6
货号 : A1324667
分子式 : C15H17ClN6O3
纯度 : 98%
分子量 : 364.787
MDL号 : MFCD22631501
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(287.84 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.71mL

2.74mL

1.37mL

27.41mL

5.48mL

2.74mL
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