46
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T23504 |
VEGFR-IN-1
VEGFR Tyrosine Kinase Inhibitor II |
Others | Others |
VEGFR inhibitor | |||
T4288 |
hVEGF-IN-1
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
hVEGF-IN-1 是一种喹唑啉衍生物,可以特异性结合内部核糖体进入位点 A 中富含 G 的序列,并会使 G-四链体结构不稳定。在 SPR 实验中,它与 IRES-A (WT) 结合的Kd 值为 0.928 μM。它能够抑制VEGF-A 蛋白表达,阻止肿瘤细胞迁移,抑制肿瘤生长。 | |||
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。 | |||
T72924 |
VEGFR-3-IN-1
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-3-IN-1 是一种新型有效且具有选择性的 VEGFR3 抑制剂,其 IC50 为 110.4 nM。VEGFR-3-IN-1 具有抗肿瘤活性,可使 VEGFR3 信号通路失活,可抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移,并且能有效抑制乳腺癌的生长。 | |||
T5466 |
Tyrosine kinase-IN-1
|
VEGFR; FGFR; FLT; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Tyrosine kinase-IN-1是一种多靶点酪氨酸激酶抑制剂,能够抑制KDR (IC50:4 nM),Flt-1 (IC50:20 nM),FGFR1 (IC50:4 nM) 和 PDGFRα (IC50:2 nM)。 | |||
T79647 |
VEGFR/PARP-IN-1
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
VEGFR/PARP-IN-1 (Compound 14b) 是一款针对VEGFR和PARP两个靶点的双重抑制剂,其对VEGFR和PARP的IC50值分别为191 nM和60.9 nM。该化合物能够抑制DNA损伤修复机制,诱导apoptosis,并使细胞在G2/M期阻滞。此外,VEGFR/PARP-IN-1对BRCA野生型乳腺癌细胞表现出较强的抗增殖效果,尤其是在MDA-MB-231和MCF-7细胞系上,其IC50值分别为4.1 μM和3.5 μM,是潜在的抗肿瘤和抗转移药物。 | |||
T79540 |
hCA/VEGFR-2-IN-1
|
Carbonic Anhydrase | Metabolism |
hCA/VEGFR-2-IN-1 是一种高效的双靶点抑制剂,对 hCA IX 和 hCA XII 两种碳酸酐酶(CA)具有极低的Ki值,分别为8.3 nM和4.7 nM。同时,hCA/VEGFR-2-IN-1 也是一种有效的 VEGFR-2 抑制剂,其 IC50 值仅为26.3 nM,并且显示出抗癌活性。 | |||
T72607 |
VEGFR-2/BRAF-IN-1
|
||
VEGFR-2/BRAF-IN-1 是一种 VEGFR-2和 BRAF 双重抑制剂,对 VEGFR-2、BRAFV600E 和BRAFWT 的IC50分别为 0.049、0.063 和 0.005 µM。VEGFR-2/BRAF-IN-1 诱导细胞凋亡,在 G1/S 期阻滞细胞周期。 | |||
T61489 | VEGFR-2/DHFR-IN-1 | ||
VEGFR-2/DHFR-IN-1 (compound 8b) 是 VEGFR-2和DHFR 的抑制剂,其IC50值分别为 0.384 和 7.881 μM。VEGFR-2/DHFR-IN-1 对大肠埃希菌,粪链球菌,肠沙门氏菌,金黄色酿脓葡萄球菌,MSSA 和MRSA 显示了良好的抗菌活性,MIC 值分别为 16,16,16,8 和 16 μg/mL。VEGFR-2/DHFR-IN-1 对 C26,HepG2 和 CF7 癌细胞系具有良好的细胞毒性,IC50值为 2.97-7.12 μM。VEGFR-2/DHFR-IN-1 可用于癌症的研究。 | |||
T80874 |
VEGFR-2/c-Met-IN-1
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2/c-Met-IN-1为VEGFR-2及c-Met的双重抑制剂,IC50值为138 nM和74 nM,显示出抗肿瘤活性。 | |||
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]。 | |||
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。 | |||
T2500 |
Cediranib
AZD2171,NSC-732208,西地尼布 |
VEGFR; FLT; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂,对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。 | |||
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。 | |||
T2624 |
OSI-930
OSI 930,噻尔非尼 |
Apoptosis; c-Fms; Raf; VEGFR; FLT; CSF-1R; Src; c-Kit | Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors |
OSI-930 是 Kit,KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂,IC50分别为 80 nM,9 nM 和 15 nM。它具有抗肿瘤活性,靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1,c-Raf 和 Lck,并且对 PDGFRα/β,Flt-3和 Abl 具有较弱的抑制活性。 | |||
T61861 |
VEGFR-2-IN-20
|
||
VEGFR-2-IN-20 (Compound 7) is a highly effective VEGFR inhibitor with significant potential for cancer research [1]. | |||
T1656L |
Vandetanib Fumarate
HSDB 8198,Zactima,Caprelsa,ZD 6474,Vandetanib |
||
Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a | |||
T61561 |
VEGFR-2-IN-18
|
||
VEGFR-2-IN-18 (Compound 15d) is a high-potency inhibitor of VEGFR-2, with an IC 50 value of 60 nM. This compound effectively initiates cell apoptosis and demonstrates significant antitumor properties [1]. | |||
T80872 |
VEGFR-2-IN-37
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-37(化合物12)是一种VEGFR-2抑制剂,其在200 μM浓度下的抑制率为56.9%。该化合物也是潜在的HUVEC增殖抑制剂。 | |||
T61229 |
VEGFR-2/DHFR-IN-2
|
||
VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1]. | |||
T61542 | VEGFR-2-IN-17 | ||
VEGFR-2-IN-17 (Compound 15a) is a highly potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), with an IC50 value of 67.25 nM. This compound exhibits significant antitumor properties [1]. | |||
T63112 |
VEGFR-IN-3
|
||
VEGFR-IN-3 (compound 3f) 是 VEGFR 抑制剂。VEGFR-IN-3 抑制 OVCAR-4 和 MDA-MB-468 癌细胞的生长,其 IC50值分别为 0.29 和 0.35 μM。VEGFR-IN-3 可用于癌症的研究。 | |||
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]. | |||
T79587 |
hCA/VEGFR-2-IN-2
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
hCA/VEGFR-2-IN-2 (compound 8g) 是一种具有吲哚酮基苯磺酰胺结构的化合物,目标是癌症相关的hCA IX/XII 及VEGFR-2 的双重抑制剂。该化合物对VEGFR-2 表现出强效的抑制作用(IC50=204 nM),且对hCAs有高亲和力,Ki 值分别为 hCA IX 3.6 nM、hCA II 16.1 nM、hCA XII 16.7 nM 以及hCA I 75.3 nM。hCA/VEGFR-2-IN-2 还展现出针对过表达VEGFR-2 的乳腺癌细胞的抗增殖活性。 | |||
T61631 |
VEGFR-2-IN-23
|
||
VEGFR-2-IN-23 (compound 11b) is a highly potent and selective inhibitor of VEGFR-2, with an impressive IC 50 value of 0.34 nM. This compound exhibits notable antitumor activity, capable of inducing apoptosis and cell cycle arrest specifically at the G1 phase [1]. | |||
T79859 |
TIE-2/VEGFR-2 kinase-IN-4
|
||
TIE-2/VEGFR-2 kinase-IN-4,一种苯并咪唑衍生物,作为有效的TIE-2和VEGFR-2酪氨酸激酶受体抑制剂,其IC50值分别为5.2 nM和5.1 nM,适用于血管生成相关研究。 | |||
T79495 |
VEGFR-2-IN-32
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-32(Comp 3a)作为一种VEGFR-2的抑制剂,其IC50值为8.93 nM。该化合物对PC-3细胞表现出细胞毒性,IC50为1.22 μM,适用于前列腺癌研究。 | |||
T81054 |
T-1-MCPAB
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
T-1-MCPAB为一种高效VEGFR-2抑制剂(IC50=0.135 µM),其显著抑制MCF7细胞迁移,适用于癌症相关研究。 | |||
T76954 | Vulinacimab | ||
Vulinacimab (HLX-06)是一款针对VEGFR-2的单克隆抗体(mAb),主要应用于癌症领域的研究。考虑到VEGFR-2在多种肿瘤中的过表达,它对于调节血管生成以及内皮细胞的增殖、存活、迁移和分化扮演着关键角色。 | |||
T79858 |
TIE-2/VEGFR-2 kinase-IN-3
|
||
TIE-2/VEGFR-2 kinase-IN-3,为苯并咪唑衍生物,具备高效的抑制作用于TIE-2与VEGFR-2受体酪氨酸激酶,其IC50值分别达到6.9 nM和3.5 nM。本化合物主要用于血管生成相关研究。 | |||
T79400 |
VEGFR-2-IN-35
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-35(compound 7)作为 VEGFR-2 抑制剂,展示出37 nM 的IC50值;同时,该化合物对MCF-7 和 HCT 116 癌细胞的抑制效果显著,IC50值分别为10.56 μM 和7.07 μM。 | |||
T78819 |
VEGFR-2-IN-33
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-33(Compound 4d)为一种有效的VEGFR抑制剂,其IC50值为61.04 nM。该化合物在抑制HepG2细胞增殖方面表现出更高的效力,IC50仅为4.31 nM,因此常用于肝细胞癌(HCC)研究领域。 | |||
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。 | |||
T79588 |
hCA/VEGFR-2-IN-3
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
hCA/VEGFR-2-IN-3(compound 8j)是一种吲哚酮基苯磺酰胺类化合物,作为hCA IX/XII和VEGFR-2的双重抑制剂,在抗癌领域具有潜在应用。该化合物对VEGFR-2表现出显著的抑制活性(IC50=358 nM),并且与hCAs有较高的亲和力,具体活性为:Ki值分别为4.2 nM(hCA IX),22.9 nM(hCA II),25.1 nM(hCA I)和28.0 nM(hCA XII)。此外,hCA/VEGFR-2-IN-3还对过表达VEGFR-2的乳腺癌细胞显示出抗增殖效果。 | |||
T79591 |
hCA/VEGFR-2-IN-4
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
hCA/VEGFR-2-IN-4 (化合物15b) 是一种具有癌症治疗潜力的吲哚酮基苯磺酰胺类双重抑制剂,旨在抑制与癌症相关的hCA IX/XII 和VEGFR-2。该化合物对VEGFR-2具有较强的抑制能力(IC50=0.811 μM),并对hCAs展现高亲和性,其Ki值分别为hCA XII的3.8 nM,hCA IX的6.2 nM,hCA II的19.8 nM,以及hCA I的35.5 nM。此外,hCA/VEGFR-2-IN-4 对于VEGFR-2过表达的乳腺癌细胞有抗增殖作用。 | |||
T76879 | Vesencumab | ||
Vesencumab (MNRP-1685A)是一种针对neuropilin-1 (NRP-1)的IG1抗体。通过与NRP-1结合,Vesencumab 阻断了NRP-1与VEGFR-2的偶联,展现出抗血管生成和抗肿瘤的活性。此化合物适用于转移性实体瘤,如卵巢癌的研究。 | |||
T9665 |
Esuberaprost Sodium
|
||
Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2]. | |||
T79403 |
VEGFR-2-IN-36
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
VEGFR-2-IN-36(compound 15)是一种具有抗癌活性的VEGFR-2抑制剂(IC50:0.067 μM)和凋亡诱导剂。该化合物能够上调BAX水平和下调Bcl-2水平,对MCF-7(IC50=0.42 μM)和HepG2(IC50=0.22 μM)癌细胞展现出明显的毒性效果。 | |||
T74422 | Sozinibercept | ||
Sozinibercept (OPT 302; VGX-300) 是VEGFR-3的可溶性形式,能有效抑制血管生成原因子VEGF-C/D 的活性,抑制血管生成和血管渗漏。Sozinibercept 对大鼠糖尿病视网膜水肿也有抑制作用。 | |||
T63967 |
Multi-kinase-IN-2
|
||
Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性,如 VEGFR-1/2/3、PDGFRα/β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化,并可诱导细胞凋亡 (apoptosis),具有抗癌作用。 | |||
T79530 |
SA-PA
|
PROTACs | PROTAC |
SA-PA是一种细胞内自组装PROTAC,以叠氮化物和炔烃为基础。它在U87细胞中可选择性降解VEGFR-2、PDGFR-β和EphB4蛋白,并可利用肿瘤组织中的内源性铜通过点击化学反应转化为PROTAC。 | |||
T79531 |
SA-VA
|
PROTACs | PROTAC |
SA-VA是一种细胞内自组装PROTAC,采用叠氮化物和炔烃基团。它能选择性地在U87细胞中降解VEGFR-2与EphB4蛋白,并可利用肿瘤组织的内源性铜促成点击反应生成PROTAC。此外,SA-VA能够促进(apoptosis)并干预S期细胞周期。 | |||
T81125 |
Sotiburafusp alfa
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Sotiburafusp alfa为一双特异性融合蛋白,由人源化VEGFR-1胞外结构域片段经101GGSGGSGGSGGSGGS115肽链与人源化IgG1-kappa 抗PD-L1重链变体L352>A、L353>A的N端(116-564)连接而成。该化合物同时具备血管生成抑制作用。 | |||
T36421 | Immuno-Oncology Screening Library | ||
The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list ... | |||
T61696 | EGFR-IN-57 | ||
EGFR-IN-57 (Compound 25a) 是一种有效的、具有口服活性的EGFR-TK 抑制剂,IC50值为 0.054 μM。EGFR-IN-57 也抑制VEGFR-2、CK2α、topoisomerase IIβ和tubulin polymerization,IC50值分别为 0.087、0.171、0.13 和 3.61 μM。EGFR-IN-57 诱导细胞 G2/M 和 pre-G1 期周期阻滞,诱导癌细胞凋亡 (apoptosis)。 | |||
T77646 |
Multi-kinase-IN-5
|
||
Multi-kinase-IN-5 (compound 15c) 是一种抑制广泛蛋白激酶的有效化合物,能够针对RET、KIT、cMet、VEGFR1、VEGFR2、FGFR1、PDGFR和BRAF展现出74%、31%、62%、40%、73%、74%、59%和69%的抑制效果。具体而言,其对FGFR1、VEGFR和RET激酶的IC50分别为1.287、0.117和1.185μM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T38250 | L-Sepiapterin | ||
L-Sepiapterin, also known as Sepiapterin, is a precursor compound crucial for the production of tetrahydrobiopterin (BH4), which serves as a coenzyme for endothelial nitric oxide synthase (eNOS). This compound demonstrates its efficacy by improving endothelial dysfunction in small mesenteric arteries from db/db mice and promoting angiogenesis. Moreover, L-Sepiapterin exerts inhibitory effects on cellular proliferation and migration in ovarian cancer cells through the down-regulation of p70S6K-de... |