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西地尼布 /Cediranib 99%+

货号:A368855 同义名: AZD2171;ZD 2171 产品仅供科研

Cediranib is a multiple RTKs inhibitor with IC50 values of <0.001μM, 0.005μM, ≤0.003μM, 0.002μM and 0.005μM for VEGFR-2, VEGFR-1, VEGFR-3, c-Kit and PDGFR-β(measured kinase activity), respectively.

Cediranib 化学结构 CAS号:288383-20-0
Cediranib 化学结构
CAS号:288383-20-0
Cediranib 3D分子结构
CAS号:288383-20-0
Cediranib 化学结构 CAS号:288383-20-0
Cediranib 3D分子结构 CAS号:288383-20-0
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Cediranib 纯度/质量文件

货号:A368855 标准纯度:99%+
批次查询: 批次纯度:

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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

PDGFR,RET 99%+
Tivozanib ++

VEGFR1, IC50: 30 nM

+++

VEGFR2, IC50: 6.5 nM

++

VEGFR3, IC50: 15 nM

99%+
Brivanib +

VEGFR1, IC50: 380 nM

++

VEGFR2, IC50: 25 nM

Flk1, 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

PDGFR,FGFR,c-Kit 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

FLT3,c-Kit 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

FLT3,c-Kit 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 99%+
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, 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

99%+
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

FLT3,RET 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。

Cediranib 生物活性

靶点
  • VEGFR1

    VEGFR1/FLT1, IC50:5 nM

  • VEGFR1

    VEGFR1/FLT1, IC50:5 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:<=3 nM

  • VEGFR3

    VEGFR3/FLT4, IC50:<=3 nM

描述 VEGF/VEGFR (vascular endothelial growth factor vascular endothelial growth factor receptor) pathway plays a key role in tumor angiogenesis by promotion of vascular and lymphatic endothelial, as well as survival, and invasion, thus resulting in neovascularization, tumor growth and metastasis. In addition, blockade of additional proangiogenic receptor tyrosine kinases, including PDGFR and FGFR, may improve long-term clinical outcomes. Cediranib is a multiple RTKs inhibitor with IC50 values of <0.001μM, 0.005μM, ≤0.003μM, 0.002μM and 0.005μM for VEGFR-2, VEGFR-1, VEGFR-3, c-Kit and PDGFR-β(measured kinase activity), respectively, less potent to PDGFR-α, CSF-1R, FGFR1, Src and Abl with IC50 values of 0.036nM, 0.11nM, 0.026nM, 0.13nM and 0.26nM, respectively. The kinase activity inhibition by Cediranib can be observed through the suppression of phosphorylation on KDR (HUVEC), c-Kit (NCI-H526), PDGFR-α (MG63), PDGFR-β (MG63), CSF-1R (NIH3T3/CSF1R) and EGFR (KB) with IC50 values of 0.0005, 0.001, 0.005, 0.008, 0.21 and 1.1μM, respectively, in cellular study. Consistent with its selectivity on VEGFR, Cediranib inhibited VEGF-stimulated HUVEC proliferation most potently with IC50 value of 0.4nM, versus IC50 values of 110nM/500nM for bFGF-/EGF-induced HUVEC proliferation, as well as 40nM PDGF-induced MG63 proliferation. Also through the inhibition of VEGFR, Cediranib inhibited vessel branching, length, and area with mean IC50 values of 0.1nM, 0.1nM and 0.2nM in in vitro study, as well as completely abolished VEGF-driven angiogenesis at 6mg/kg/day in in vivo models. The effect of Cediranib-induced hypertrophy in bone growth plate and inhibition on luteal development in ovary (5mg/kg, orally) further confirmed its inactivation of VEGF-induced angiogenesis within complex physiologic settings. Cediranib showed broad-spectrum anti-tumor activity as oral administration of Cediranib at dose of 1.5,3 and 6mg/kg once daily inhibited growth of all human tumor xenografts examined, including SW620 (colon), Calu-6 (lung), PC-3 (prostate), MDA-MB-231 (breast) and SKOV-3 (ovary), with vascular regression observed in Calu-6 lung tumor xenografts at dose of 6mg/kg[1].
作用机制 Cediranib is an ATP-competitive inhibitor of KDR tyrosine kinase.[1]

Cediranib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
HUVEC cell Proliferation assay 3 days Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay, ED50=12 nM 19101155

Cediranib 动物研究

Dose Mice: 1.5 mg/kg, 3 mg/kg[1] (p.o.), 1 mg/kg - 25 mg/kg[2] (p.o.); 0.75 mg/kg - 5 mg/kg[3] (i.p.)
Administration p.o., i.p.

Cediranib 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
NCT00691730 Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 << Not Applicable Active, not recruiting December 2018 Canada, Alberta ... 展开 >> Tom Baker Cancer Centre Calgary, Alberta, Canada, T2N 4N2 Canada, Ontario London Regional Cancer Program London, Ontario, Canada, N6A 4L6 Mount Sinai Hospital Toronto, Ontario, Canada, M5G 1X5 University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT00310089 Breast Cancer Not Applicable Completed - United States, Maryland ... 展开 >> Warren Grant Magnuson Clinical Center - NCI Clinical Studies Support Bethesda, Maryland, United States, 20892-1182 United States, New Jersey Cancer Institute of New Jersey at UMDNJ - Robert Wood Johnson Medical School New Brunswick, New Jersey, United States, 08903 收起 <<
NCT02910843 Rectal Cancer Phase 1 Recruiting December 2022 Switzerland ... 展开 >> St. Claraspital Basel Recruiting Basel, Switzerland, 4016 Contact: Dieter Köberle, MD    +41 61 685 85 85    dieter.koeberle@claraspital.ch    Principal Investigator: Dieter Köberle, MD          Universitätsspital Basel Recruiting Basel, Switzerland, 4031 Contact: Viviane Hess, Prof    +41 61 265 50 74    viviane.hess@usb.ch    Principal Investigator: Viviane Hess, Prof          Inselspital Bern Recruiting Bern, Switzerland, 3010 Contact: Martin D. Berger, MD    +41 31 632 41 14    martin.berger@insel.ch    Principal Investigator: Martin D. Berger, MD          Kantonsspital Graubünden Recruiting Chur, Switzerland, 7000 Contact: Ioannis Metaxas, MD    +41 81 256 66 46    ioannis.metaxas@ksgr.ch    Principal Investigator: Ioannis Metaxas, MD          Kantonsspital Luzern Recruiting Luzern, Switzerland, 6000 Contact: Ralph Winterhalder, MD    +41 41 205 58 75    ralph.winterhalder@ksl.ch    Principal Investigator: Ralph Winterhalder, MD          Kantonsspital St. Gallen Recruiting St. Gallen, Switzerland, 9007 Contact: Markus Jörger, MD    +41 71 494 29 22    markus.joerger@kssg.ch    Principal Investigator: Markus Jörger, MD          UniversitätsSpital Zürich Recruiting Zurich, Switzerland, 8091 Contact: Bernhard Pestalozzi, Prof    +41 (0)44 255 34 40    bernhard.pestalozzi@usz.ch    Principal Investigator: Bernhard Pestalozzi, Prof 收起 <<

Cediranib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL

Cediranib 技术信息

CAS号288383-20-0
分子式C25H27FN4O3
分子量450.505
别名 AZD2171;ZD 2171;NSC-732208
运输蓝冰
存储条件

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

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 18 mg/mL(39.96 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
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