切换导航

Apatinib

现货
Catalog No.
B2303
VEGFR2选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
5mg
¥ 1,280.00
现货
10mg
¥ 1,430.00
现货
25mg
¥ 2,380.00
现货
50mg
¥ 3,330.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Apatinib (YN968D1)is a potent inhibior of the VEGF signaling pathway with the IC50 value of 1nM for VEGFR-2 in in vitro enzyme experiments [1].

In vitro, Apatinib has shown the inhibition of tyrosine kinase activities with the IC50 values of 0.013μM, 0.429μM and 0.53μM for Ret, c-kit and c-src, respectively. In addition, Apatinib has been revealed to have no significant effects in EGFR, Her-2 or FGFR1 in concentrations up to 10μM. Apart from these, Apatinib has been reported to inhibit the growth factor-stimulated receptor phosphorylation at the cellular level. Furthermore, Apatinib has also reported to slightly inhibitor proliferation of HUVEC by 20% FBS with the IC50 value of 23.4μM and significantly inhibit stimulated by 20ng/mL VEGF with the IC50 value of 0.17μM. Once-daily oral administration of Apatinib has been noted to produce a dose-dependent inhibition of tumor growth in human tumor xenografts in immunodeficient mice [1]

References:
[1] Tian S1, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.

.

文献引用

1. Zhong W, Jin W, et al. "Pioglitazone Induces Cardiomyocyte Apoptosis and Inhibits Cardiomyocyte Hypertrophy Via VEGFR-2 Signaling Pathway." Arq Bras Cardiol. 2018 Jul 2. pii: S0066-782X2018005008102. PMID:29972411

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt493.58
Cas No.811803-05-1
FormulaC25H27N5O4S
Solubility≥49.4mg/mL in DMSO
Chemical NameN-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide;methanesulfonic acid
SDFDownload SDF
Canonical SMILESCS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

HUVEC(人脐静脉内皮细胞)

制备方法

溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

37℃

实验结果

在HUVEC中,Apatinib以浓度依赖性方式降低VEGF刺激的VEGFR-2 KDR的磷酸化。0.1 μM的浓度完全抑制VEGFR-2活化。此外,在相关配体刺激的Mo7e和NIH-3T3细胞中,Apatinib以浓度依赖性方式消除c-kit和PDGFRb的磷酸化。此外,Apatinib在体外抑制HUVEC的增殖、迁移和管形成,阻断大鼠主动脉环出芽。

动物实验: [1]

动物模型

人肿瘤异种移植物裸鼠

给药剂量

每天一次,口服

制备方法

在0.5%(w / v)羧甲基纤维素和5%(w / v)葡萄糖溶液中稀释。

实验结果

在NCI-H460人肺肿瘤、HCT 116人结肠肿瘤或SGC-7901人胃肿瘤荷瘤裸鼠中,Apatinib抑制肿瘤生长。Apatinib和docetaxel或oxaliplatin共同使用对NCI-H460和Ls174t异种移植物发挥协同的肿瘤生长抑制作用。Apatinib还显著抑制NCI-H460异种移植肿瘤组织中的血管生成。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

1. Tian S, Quan H, Xie C et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.

生物活性

描述 Apatinib是一种具有口服生物有效性的VEGFR2选择性抑制剂, IC50值为1 nM。
靶点 VEGFR2 RET c-Kit c-Src PDGFRα  
IC50 1 nM 13 nM 429 nM 530 nM >1 μM  

质量控制

化学结构

Apatinib

相关生物数据

Apatinib