Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9724 |
VEGFR2-IN-2
|
Others | Others |
VEGFR2-IN-2 具有抗炎和镇痛活性。 | |||
T40581 |
TIE-2/VEGFR-2 kinase-IN-2
|
||
TIE-2/VEGFR-2 kinase-IN-2 is a powerful inhibitor of both VEGFR2 and Tie-2 kinases, displaying noteworthy pIC 50 values of 8.61 and 8.56, respectively. This compound acts as an anti-angiogenic agent, making it highly relevant for cancer research. | |||
T8817 |
TIE-2/VEGFR-2 kinase-IN-1
|
||
TIE-2/VEGFR-2 kinase-IN-1 用于合成TIE-2或者VEGFR-2抑制剂,可用于研究不适当的血管生成的相关疾病。 | |||
T9979 |
VEGFR-2-IN-29
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-29是一种 VEGFR2抑制剂。 | |||
T37078 |
VEGFR-2-IN-6
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-6(WO 02/059110)是一种 VEGFR2 的强效抑制剂,这是一种在血管生成调控中起关键作用的受体[1]。 | |||
T3980 |
Su1498
Tyrphostin SU 1498,AG 1498 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Su1498 (Tyrphostin SU 1498) 是一种选择性的 VEGFR2 抑制剂,能够抑制 Flk-1 (IC50:700 nM)。 | |||
T5475 |
ZD-4190
|
EGFR; VEGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
ZD-4190 是血管内皮细胞生长因子受体 2 (VEGFR2) 和表皮生长因子受体 (EGFR) 信号传导的抑制剂,用于治疗癌症。 | |||
T2576 |
Brivanib (alaninate)
丙氨酸布立尼布,BMS-582664,Brivanib Alaninate |
VEGFR; FGFR; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Brivanib Alaninate (BMS-582664) 是一种血管内皮生长因子受体 2 (VEGFR2) 抑制剂的丙氨酸盐,IC50值为 25 nM,具有潜在的抗肿瘤活性。它对 VEGFR1 和 FGFR1 适度抑制,对 VEGFR2 的选择性是对 PDGFRβ 的 240 倍。 | |||
T2056 |
VEGFR-2-IN-5
2, 4-Pyrimidinediamine with linker,UNC0064-12,2,4-Pyrimidinediamine with linker |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-5 (UNC0064-12) 是 VEGFR2 抑制剂。 | |||
T4425 |
JK-P3
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
JK-P3 是广谱 VEGFR2抑制剂。它能够抑制 VEGF-A 刺激的 VEGFR2 激活和细胞内信号转导,也可阻碍内皮单层细胞迁移和血管生成,影响成纤维细胞生长因子受体激酶在体外的活性。它具有抗血管生成的作用。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
T2054 |
Altiratinib
DCC-2701 |
VEGFR; Tie-2; FLT; Trk receptor; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Altiratinib (DCC-2701) 是一种多靶点激酶抑制剂,能够抑制 MET (IC50:2.7 nM),TIE2 (IC50:8 nM),VEGFR2 (IC50:9.2 nM),FLT3 (IC50:9.3 nM),Trk1 (IC50:0.85 nM),Trk2 (IC50:4.6 nM) 和 Trk3 (IC50:0.83 nM)。 | |||
T37424 |
CAY10781
CAY10781 |
Others | Others |
CAY10781 是一种神经纤毛蛋白-1 (NRP-1) 和 VEGF-A.1 之间蛋白质-蛋白质相互作用的抑制剂。当使用浓度为 12.5 μM 时,它可抑制 43% 的相互作用。 当以相同浓度使用时,CAY10781 还抑制 VEGF-A 诱导的儿茶酚胺 A 分化 (CAD) 细胞中 VEGFR2 的磷酸化。 | |||
T0097L |
Pazopanib
帕唑帕尼,GW786034 |
VEGFR; FGFR; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Pazopanib (GW786034) 是一种小分子抑制剂,可抑制多种具有潜在抗肿瘤活性的蛋白酪氨酸激酶。它抑制VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1和c-Fms 的IC50分别为10、30、47、84、74、140和146 nM。 | |||
T6517 |
Golvatinib
E-7050,戈伐替尼 |
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Golvatinib (E-7050) 是一种 c-Met (IC50:14 nM) 和 VEGFR2 (IC50:16 nM) 的双重抑制剂。 | |||
T61943 | VEGFR-2-IN-5 hydrochloride | ||
VEGFR-2-IN-5 hydrochloride 是有效的VEGFR2抑制剂。 | |||
T64215 |
FGFR3-IN-2
|
||
FGFR3-IN-2 (compound 18b) 是一种有效的、选择性的 FGFR3 抑制剂,能够抑制 FGFR3 (IC50: 4.1 nM) 和 VEGFR2 (IC50: 570 nM)。FGFR3-IN-2 能够用于研究膀胱癌。 | |||
T10123 |
VEGFR-2-IN-9
KDR-in-4 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-9 (KDR-in-4) 是一种高效的 KDR/VEGFR2 抑制剂(IC50:7 nM),可用于研究乳腺癌。 | |||
T68546 |
PF-00337210
|
||
PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may even... | |||
T37079 |
VEGFR2 Kinase Inhibitor II
|
||
Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. V... | |||
T61038 | VEGFR-2-IN-10 | ||
VEGFR-2-IN-10 对 VEGF 诱导的VEGFR2磷酸化表现出增强的抗血管生成效力,IC50值为 0.7 μM,而无细胞毒性作用。 | |||
T71187 |
Foretinib phosphate
|
||
Foretinib phosphate is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. | |||
T61137 | VEGFR-2-IN-19 | ||
VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis. Its mechanism of action involves the induction of cellular apoptosis and elevation of intracellular reactive oxygen species. Due to these properties, VEGFR-2-IN-19 holds promise as an effective anticancer agent [1]. | |||
T80873 |
VEGFR2/HDAC1-IN-1
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR2/HDAC1-IN-1(compound 13)是一款有效的VEGFR-2和HDAC双重抑制剂,其IC50值分别为57.83 nM 和9.82 nM 。该化合物能够阻滞细胞周期于S期及G2期,并能诱导HeLa细胞发生凋亡,同时具有抗血管生成的特性。 | |||
T76506 |
Coibamide A
|
||
Coibamide A 是一种 N-甲基稳定的细胞毒性缩酚肽,具有强大的抗增殖活性。Coibamide A 通过mTOR 独立机制诱导自噬体积累。Coibamide A 诱导细胞凋亡。Coibamide A 抑制VEGFA/VEGFR2表达并抑制胶质母细胞瘤异种移植物中的肿瘤生长。 | |||
T81739 |
Multi-target kinase inhibitor 2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Multi-target kinase inhibitor 2 (compound 5K) 作为一种multi-targeted kinase抑制剂,对EGFR、Her2、VEGFR2和CDK2酶表现出强效活性,IC50值在40至204 nM之间。此化合物对包括HepG2、HeLa、MDA-MB-231 和 MCF-7在内的多种细胞系均显示出显著的细胞毒性,其IC50值分别为41、57、51 和 59 μM。此外,Multi-target kinase inhibitor 2 还能诱导HepG2细胞发生周期阻滞和凋亡 (apoptosis)。 | |||
T83911 |
CYY292
|
||
CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。 | |||
T68389 | LY2457546 | ||
LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge... |