Ambeed.cn

首页 / 抑制剂/激动剂 / / VEGFR / Apatinib

Apatinib {[allProObj[0].p_purity_real_show]}

货号:A314938 同义名: YN968D1; Rivoceranib

Apatinib is a selective inhibitor of VEGFR2 with IC50 of 1 nM.

Apatinib 化学结构 CAS号:811803-05-1
Apatinib 化学结构
CAS号:811803-05-1
Apatinib 3D分子结构
CAS号:811803-05-1
Apatinib 化学结构 CAS号:811803-05-1
Apatinib 3D分子结构 CAS号:811803-05-1
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Apatinib 纯度/质量文件 产品仅供科研

货号:A314938 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

更多 >
产品名称 VEGFR1 VEGFR2 VEGFR3 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

++++

VEGFR2, IC50: 3 nM

VEGFR2/Flk1, IC50: 3 nM

+++

VEGFR3, IC50: 6 nM

RET,PDGFR 99% (HPLC)
Tivozanib ++

VEGFR1, IC50: 30 nM

+++

VEGFR2, IC50: 6.5 nM

++

VEGFR3, IC50: 15 nM

99%+
Brivanib +

VEGFR1, IC50: 380 nM

++

Flk1, IC50: 25 nM

VEGFR2, IC50: 25 nM

99%+
Regorafenib +++

VEGFR1, IC50: 13 nM

+++

VEGFR2, IC50: 4.2 nM

+

VEGFR3, IC50: 46 nM

RET 98%
Pazopanib +++

VEGFR1, IC50: 10 nM

++

VEGFR2, IC50: 30 nM

+

VEGFR3, IC50: 47 nM

c-Kit,FGFR,PDGFR 99%
Sitravatinib +++

VEGFR1 (FLT1), IC50: 6 nM

+++

VEGFR2 (KDR), IC50: 5 nM

++++

VEGFR3 (FLT4), IC50: 2 nM

99%+
Foretinib +++

VEGFR1/FLT1, IC50: 6.8 nM

++++

KDR, IC50: 0.86 nM

++++

VEGFR3/FLT4, IC50: 2.8 nM

Tie-2 99%+
MGCD-265 analog ++++

VEGFR1, IC50: 3 nM

++++

VEGFR2, IC50: 3 nM

++++

VEGFR3, IC50: 4 nM

Tie-2 99%+
Lactate +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

c-Kit,FLT3 85%
AEE788 +

FLT1, IC50: 59 nM

+

KDR, IC50: 77 nM

EGFR 98+%
Linifanib ++++

VEGFR1/FLT1, IC50: 3 nM

++++

VEGFR2/KDR, IC50: 4 nM

+

VEGFR3/FLT4, IC50: 190 nM

FLT3 99%+
Vatalanib 2HCl +

VEGFR1/FLT1, IC50: 77 nM

++

VEGFR2/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

+

VEGFR3/FLT4, IC50: 660 nM

c-Fms,c-Kit 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 nM

98%
Dovitinib +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

c-Kit,FLT3 99%+
ZM 306416 +

VEGFR1, IC50: 0.33 μM

Src 99%+
KRN-633 +

VEGFR1, IC50: 170 nM

+

VEGFR2, IC50: 160 nM

+

VEGFR3, IC50: 125 nM

BTK,c-Kit 98%
OSI-930 +++

FLT1, IC50: 8 nM

+++

KDR, IC50: 9 nM

99%+
Lenvatinib ++

VEGFR1/FLT1, IC50: 22 nM

++++

VEGFR2/KDR, IC50: 4.0 nM

+++

VEGFR3/FLT4, IC50: 5.2 nM

98%
NVP-BAW2881 +

hVEGFR1, IC50: 820 nM

+++

mVEGF2, IC50: 165 nM

hVEGFR2, IC50: 9 nM

+

hVEGFR3, IC50: 420 nM

99%
Cediranib +++

VEGFR1/FLT1, IC50: 5 nM

++++

VEGFR2/KDR, IC50: 0.5 nM

c-Kit 99%+
Nintedanib ++

VEGFR1, IC50: 34 nM

+++

VEGFR2, IC50: 13 nM

+++

VEGFR3, IC50: 13 nM

FLT3 99+%
BMS-794833 ++

VEGFR2, IC50: 15 nM

99%+
SKLB1002 ++

VEGFR2, IC50: 32 nM

99%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 99%
SU 5402 ++

VEGFR2, IC50: 20 nM

98%
Rivoceranib Mesylate ++++

VEGFR2, IC50: 1 nM

RET 98+%
Ponatinib ++++

VEGFR2, IC50: 1.5 nM

98%
LY2874455 +++

VEGFR2, IC50: 7 nM

99%+
ZM323881 HCl ++++

VEGFR2, IC50: <2 nM

98%
AZD2932 +++

VEGFR-2, IC50: 8 nM

c-Kit 99%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

98%
Sorafenib ++

VEGFR2, IC50: 90 nM

VEGFR2/Flk1, IC50: 90 nM

99%
CYC-116 ++

VEGFR2, Ki: 44 nM

FLT3 99%+
Golvatinib ++

VEGFR2, IC50: 16 nM

99%+
Sunitinib +

VEGFR2 , IC50: 80 nM

FLT3 98%
RAF265 ++

VEGFR2, EC50: 30 nM

99%+
PD173074 99%+
BFH772 ++++

VEGFR2, IC50: 3 nM

98%
Semaxinib +

VEGFR2/Flk1, IC50: 1.23 μM

98%
Vandetanib ++

VEGFR2, IC50: 40 nM

+

VEGFR3, IC50: 110 nM

EGFR 99%
SAR131675 ++

VEGFR3, IC50: 23 nM

99%+
ENMD-2076 +

VEGFR2/KDR, IC50: 58.2 nM

++

VEGFR3/FLT4, IC50: 15.9 nM

RET,FLT3 98%
Telatinib +++

VEGFR2, IC50: 6 nM

++++

VEGFR3, IC50: 4 nM

c-Kit 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Apatinib 生物活性

描述 Vascular endothelial growth factor (VEGF) regulates angiogenesis and endothelial cell function via binding to three membrane receptor tyrosine kinases: VEGFR‐1, VEGFR‐2, and VEGFR‐3. Apatinib is a selective inhibitor of VEGFR‐2 with an IC50 value of 1 nM. The kinase activities of Ret, c-Kit and c-Src tyrosine kinases could also be potently inhibited by apatinib with IC59 values of 0.013, 0.429 and 0.53 μM, respectively. In human umbilical vein endothelial cells (HUVEC), apatinib decreased VEGF‐stimulated activation of VEGFR‐2/KDR at a dose-dependent manner, and complete inhibition of VEGFR‐2/KDR phosphorylation was observed when 0.1 μM apatinib was applied. Apatinib at 0.01 – 10 μM also suppressed the activation of c‐kit and PDGFRβ in Mo7e and NIH‐3T3 cells. The proliferation of HUVEC induced by 20% FBS was inhibited by apatinib with an IC50 value of 23.4 μM, and the proliferation stimulated by 20 ng/mL VEGF was significantly blocked by apatinib with an IC50 value of 0.17 μM. Apatinib at 1 μM prevented HUVEC from forming the tubes and significantly inhibited FBS-triggered cell migration. Two-week oral administration of apatinib (100 and 200 mg/kg/day, once per day) significantly inhibited tumor growth in immunodeficient mice implanted with human tumor xenografts. In mice implanted with NCI‐H460 tumor, the antitumor effect of apatinib (150 mg/kg/day) alone was enhanced by the combination with docetaxel (12 mg/kg), showing 93% inhibition after two weeks of treatment[3].
作用机制 Apatinib is a small antiangiogenic molecule that specifically binds to the phosphorylation sites of VEGFR-2, inhibiting VEGF binding and subsequent VEGFR-2 autophosphorylation[4].

Apatinib 动物研究

Dose Mice: 37.5 mg/kg - 150 mg/kg[3] (p.o.); 100 mg/kg - 300 mg/kg[4] (p.o.)
Administration p.o.

Apatinib 参考文献

[1]Tian S, Quan H, 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.

[2]Mi YJ, Liang YJ, et al. Apatinib (YN968D1) reverses multidrug resistance by inhibiting the efflux function of multiple ATP-binding cassette transporters. Cancer Res. 2010 Oct 15;70(20):7981-91.

[3]Tian S, 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.

[4]Zhang H. Apatinib for molecular targeted therapy in tumor. Drug Des Devel Ther. 2015 Nov 13;9:6075-81.

Apatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

Apatinib 技术信息

CAS号811803-05-1
分子式C24H23N5O
分子量 397.47
SMILES Code O=C(NC1=CC=C(C2(C#N)CCCC2)C=C1)C3=C(NCC4=CC=NC=C4)N=CC=C3
MDL No. MFCD21648511
别名 YN968D1; Rivoceranib
运输蓝冰
InChI Key WPEWQEMJFLWMLV-UHFFFAOYSA-N
Pubchem ID 11315474
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。