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CP-547632 {[allProObj[0].p_purity_real_show]}

货号:A867793

CP-547632是VEGFR-2和基础成纤维细胞生长因子(FGF)激酶的强效抑制剂,IC50分别为11 nM和9 nM,具有对表皮生长因子受体、血小板源生长因子及其他相关酪氨酸激酶的选择性。它还可以抑制VEGF刺激的VEGFR-2自磷酸化,IC50值为6 nM。

CP-547632 化学结构 CAS号:252003-65-9
CP-547632 化学结构
CAS号:252003-65-9
CP-547632 3D分子结构
CAS号:252003-65-9
CP-547632 化学结构 CAS号:252003-65-9
CP-547632 3D分子结构 CAS号:252003-65-9
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CP-547632 纯度/质量文件 产品仅供科研

货号:A867793 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

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,PDGFR,FGFR 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/Flk1, IC50: 270 nM

VEGFR2/KDR, IC50: 37 nM

+

VEGFR3/FLT4, IC50: 660 nM

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

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/Flk1, IC50: 0.18 nM

VEGFR2/KDR, IC50: 0.2 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

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/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 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。

CP-547632 生物活性

描述 CP-547632 is an orally active, ATP-competitive inhibitor that potently targets VEGFR-2 and FGF kinases, with IC50 values of 11 nM and 9 nM, respectively. It exhibits selectivity for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 demonstrates antitumor efficacy[1].
体内研究

CP-547632 (oral administration; 6.25-100 mg/kg/day; for 10-24 days) induces dose-dependent inhibition of tumor growth in Colo-205, DLD-1, and MDA-MB-231 xenografts[1].

CP-547632 (oral; 50 mg/kg; a single oral dose) achieves plasma concentrations exceeding 500 ng/ml for 12 hours[1].

体外研究

CP-547632 (1-1000 nM; 1 hour) dose-dependently suppresses VEGF-induced phosphorylation of VEGFR-2, with an IC50 value of 6 nM[1].

CP-547632 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
NCT00074854 Lung Neoplasms Phase 1 Phase 2 Completed - United States, California ... 展开 >> Pfizer Investigational Site Greenbrae, California, United States, 94904 Pfizer Investigational Site San Mateo, California, United States, 94402 Pfizer Investigational Site San Pablo, California, United States, 94806 United States, Florida Pfizer Investigational Site Tampa, Florida, United States, 33612-9497 United States, Louisiana Pfizer Investigational Site Covington, Louisiana, United States, 70433 Pfizer Investigational Site Metairie, Louisiana, United States, 70002 Pfizer Investigational Site Metairie, Louisiana, United States, 70006 Pfizer Investigational Site New Orleans, Louisiana, United States, 70115 United States, Massachusetts Pfizer Investigational Site Boston, Massachusetts, United States, 02215 United States, New York Pfizer Investigational Site Stony Brook, New York, United States, 11794 United States, Pennsylvania Pfizer Investigational Site Philadelphia, Pennsylvania, United States, 19111 United States, Tennessee Pfizer Investigational Site Gallatin, Tennessee, United States, 37066 Pfizer Investigational Site Hermitage, Tennessee, United States, 37076 Pfizer Investigational Site Lebanon, Tennessee, United States, 37087 Pfizer Investigational Site Murfreesboro, Tennessee, United States, 37130 Pfizer Investigational Site Nashville, Tennessee, United States, 37203 Pfizer Investigational Site Nashville, Tennessee, United States, 37205 Pfizer Investigational Site Nashville, Tennessee, United States, 37207 Pfizer Investigational Site Nashville, Tennessee, United States, 37211 Pfizer Investigational Site Smyrna, Tennessee, United States, 37167 收起 <<
NCT00096239 Fallopian Tube Cancer ... 展开 >> Ovarian Cancer Primary Peritoneal Cavity Cancer 收起 << Phase 2 Completed - United States, California ... 展开 >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095-1781 收起 <<
NCT00074867 Ovarian Neoplasms ... 展开 >> Peritoneal Neoplasms Fallopian Tube Neoplasms 收起 << Phase 2 Completed - United States, California ... 展开 >> Pfizer Investigational Site Los Angeles, California, United States, 90095 Pfizer Investigational Site Santa Monica, California, United States, 90404 United States, Maryland Pfizer Investigational Site Baltimore, Maryland, United States, 21237 United States, Massachusetts Pfizer Investigational Site Boston, Massachusetts, United States, 02114 Pfizer Investigational Site Boston, Massachusetts, United States, 02115 Pfizer Investigational Site Boston, Massachusetts, United States, 02215 United States, New York Pfizer Investigational Site New York, New York, United States, 10016 Canada, Ontario Pfizer Investigational Site Hamilton, Ontario, Canada, L8V 5C2 Canada Pfizer Investigational Site Quebec, Canada, G1R 2J6 收起 <<

CP-547632 参考文献

[1]Beebe JS, et al. Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res. 2003 Nov 1;63(21):7301-9.

CP-547632 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

CP-547632 技术信息

CAS号252003-65-9
分子式C20H24BrF2N5O3S
分子量 532.4
SMILES Code NC(=O)C1=C(NC(=O)NCCCCN2CCCC2)SN=C1OCC1=C(F)C=C(Br)C=C1F
MDL No. MFCD07772279
别名
运输蓝冰
InChI Key HXHAJRMTJXHJJZ-UHFFFAOYSA-N
Pubchem ID 9811611
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 105 mg/mL(197.22 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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