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。
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 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
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。 |
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]. |
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 << |
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 |
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 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
|