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Foretinib {[allProObj[0].p_purity_real_show]}

货号:A169062 同义名: XL880;GSK1363089

Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Foretinib is less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and with little activity to FGFR1 and EGFR.

Foretinib 化学结构 CAS号:849217-64-7
Foretinib 化学结构
CAS号:849217-64-7
Foretinib 3D分子结构
CAS号:849217-64-7
Foretinib 化学结构 CAS号:849217-64-7
Foretinib 3D分子结构 CAS号:849217-64-7
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Foretinib 纯度/质量文件 产品仅供科研

货号:A169062 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 VEGFR1 VEGFR2 VEGFR3 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

++++

VEGFR2/Flk1, IC50: 3 nM

VEGFR2, IC50: 3 nM

+++

VEGFR3, IC50: 6 nM

PDGFR,RET 98%
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-Kit,c-Fms 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

c-Kit,BTK 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

98%
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

98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 98+%
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 98%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

98%
Sorafenib ++

VEGFR2/Flk1, IC50: 90 nM

VEGFR2, 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 98%
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。

Foretinib 生物活性

靶点
  • VEGFR1

    VEGFR1/FLT1, IC50:6.8 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:2.8 nM

  • VEGFR2

    KDR, IC50:0.86 nM

描述 The overexpression and activation of the Met receptor and its ligand HGF (hepatocyte growth factor) are associated with a wide variety of human malignancies. Meanwhile, it is found that VEGFRs can cooperate with Met to induce tumor invasion and vascularization. Foretinib is a multiple RTKs inhibitor with IC50 values of 0.4, 0.9/2.8 and 3nM for Met, VEGFR2/3 and Ron, less potent to Tie-2, Flt-3, PDGFRα, KIT, VEGFR1, PDGFRβ with IC50 values of 1.1nM, 3.6nM, 3.6nM, 6.7nM, 6.8nM and 9.6nM, with almost no inhibition of FGFR1 or EGFR (measured by in vitro kinase assay). Potent inhibition of p-Met by Foretinib with IC50 values of 23 and 21nM in PC-3 and B16F10 cells, as well as the suppression of p-ERK and p-VEGFR2 induced by VEGF with IC50 of 16nM in HUVECs can be observed, suggesting the cellular RTKs inhibition. Foretinib can block HGF-induced migration with IC50 value of 44nM, as well as inhibit the anchorage-independent tumor cell colony growth of B16F10 cells with IC50 of 40nM. A further study on Inhibition of endothelial tubule formation and migration by Foretinib showed that Foretinib at concentration of 5nM or higher can both inhibit VEGF-induced tubule formation and block VEGF- or HGF-stimulated migration of HMVEC-L cells. Once daily oral administration of Foretinib at dose of 30 and 100mg/kg reduced lung surface tumor burden by 50% and 58%, respectively, in mice intravenously implanted B16F10 cells. Similarly, Foretinib at dose of 30 and 100mg/kg resulted in tumor growth inhibition of 64% and 87%, respectively, in mice bearing B16F10 solid tumors[1].
作用机制 Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR.[1]

Foretinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A172 100/300/900 nM Function Assay 1 h inhibits the phosphorylation of MerTK  24658326
A172 100/300/900 nM Function Assay 1 h inhibits the activity of Axl, Tyro3 24658326
A172 100/300/900 nM Function Assay 1 h decreases Akt phosphorylation in a concentration dependent manner 24658326
A172 100/300/900 nM Growth Inhibition Assay 48 h reduces cell survival at 900 nM significantly 24658326

Foretinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01068587 Lung Cancer Phase 1 Phase 2 Completed - Canada, British Columbia ... 展开 >> BCCA - Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Juravinski Cancer Centre at Hamilton Health Sciences Hamilton, Ontario, Canada, L8V 5C2 Ottawa Health Research Institute - General Division Ottawa, Ontario, Canada, K1H 8L6 Univ. Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT00725712 Neoplasms, Gastrointestinal Tr... 展开 >>act 收起 << Phase 2 Completed - United States, Alabama ... 展开 >> GSK Investigational Site Birmingham, Alabama, United States, 35294 United States, Arizona GSK Investigational Site Scottsdale, Arizona, United States, 85258 United States, California GSK Investigational Site Los Angeles, California, United States, 90024 GSK Investigational Site Stanford, California, United States, 94305 United States, District of Columbia GSK Investigational Site Washington, D.C., District of Columbia, United States, 20007 United States, Georgia GSK Investigational Site Atlanta, Georgia, United States, 30309 United States, Illinois GSK Investigational Site Chicago, Illinois, United States, 60637 United States, Massachusetts GSK Investigational Site Boston, Massachusetts, United States, 02114 United States, Michigan GSK Investigational Site Detroit, Michigan, United States, 48201 United States, Montana GSK Investigational Site Billings, Montana, United States, 59101 United States, New Mexico GSK Investigational Site Albuquerque, New Mexico, United States, 87131 United States, New York GSK Investigational Site New York, New York, United States, 10016 GSK Investigational Site New York, New York, United States, 10021 United States, North Carolina GSK Investigational Site Durham, North Carolina, United States, 27710 United States, Oregon GSK Investigational Site Portland, Oregon, United States, 97239 United States, Texas GSK Investigational Site Austin, Texas, United States, 78705 United States, Wisconsin GSK Investigational Site Madison, Wisconsin, United States, 53792 收起 <<
NCT00725712 - Completed - -

Foretinib 参考文献

[1]Qian F, Engst S, et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res. 2009;69(20):8009-16.

Foretinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.58mL

0.32mL

0.16mL

7.90mL

1.58mL

0.79mL

15.81mL

3.16mL

1.58mL

Foretinib 技术信息

CAS号849217-64-7
分子式C34H34F2N4O6
分子量 632.654
别名 XL880;GSK1363089;EXEL-2880;GSK089
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 80 mg/mL(126.45 mM),配合低频超声助溶,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

30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension

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