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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9929 |
Ramucirumab
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Ramucirumab 是一种人 VEGFR-2 拮抗剂,具有抗实体瘤活性。它是人源化单克隆抗体,能够与 VEGFR-2 结合,阻碍 VEGFR 配体 VEGF-A,VEGF-C 和 VEGF-D 结合。 | |||
T7123 |
AMG-47a
|
VEGFR; p38 MAPK; JAK; Src | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells; Tyrosine Kinase/Adaptors |
AMG-47a 是具有口服活性的 Lck 抑制剂,IC50值为 0.2 nM。它具有抗炎作用,对 VEGF2、p38α、p38α、Jak3、MLR 和 IL-2的 IC50值分别为 1、3、72、30 和 21 nM。 | |||
T1792L |
Regorafenib monohydrate
|
Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Regorafenib monohydrate 是一种新型口服多激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。 | |||
T2456 |
Tivozanib
替沃扎尼,AV-951,KRN951 |
VEGFR; PDGFR; Ephrin Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Tivozanib (KRN951) 是一种选择性的 VEGFR 1/2/3抑制剂,它们的 IC50值分别为0.21 nM、0.16 nM、0.24 nM。 | |||
T6351 |
MGCD-265 analog
MGCD-265,Glesatinib |
Apoptosis; VEGFR; c-Met/HGFR | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
MGCD-265 analog (Glesatinib) 是一种口服生物可利用的多靶点酪氨酸激酶抑制剂,具有抗肿瘤活性,对 c-Met 和 VEGFR2 的 IC50 分别为 29 nM 和 10 nM。 | |||
T1792 |
Regorafenib
BAY 73-4506,瑞戈非尼,Fluoro-Sorafenib,瑞格非尼 |
Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5/2.5/4.2/7/13/22 nM),具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。 | |||
T2514 |
Linifanib
利尼伐尼,ABT-869,RG3635,AL-39324 |
Apoptosis; c-Fms; VEGFR; FLT; CSF-1R; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; Tyrosine Kinase/Adaptors |
Linifanib (AL-39324) 是一种高效口服的VEGFR 和PDGFR 家族多靶点抑制剂,具有显著的抗肿瘤活性。它对无关 RTKs、可溶性酪氨酸激酶或丝氨酸/苏氨酸激酶的活性要低得多。它是特异性 miR-10b 抑制剂,阻断miR-10b 的生物合成。 | |||
T60396 |
JMS-053
|
Phosphatase | Metabolism |
JMS-053 是一种具有有效性和选择性的磷酸酶 DUSP3 抑制剂, 抑制 PTP4A3、 PTP4A1 、 PTP4A2 和 CDC25B,抑制癌细胞迁移和球体生长,避免血管内皮生长因子或脂多糖对微血管内皮屏障功能的破坏。 | |||
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。 | |||
T2064 |
Semaxinib
司马沙尼,SU5416 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Semaxinib (SU5416) 是一种选择性的 VEGFR(Flk-1/KDR) 抑制剂,其 IC50=1.23 μM。 | |||
T68455 |
AP23846
AP-23846 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
AP23846 是一种新型高效的 Src 家族激酶抑制剂,可降低人实体瘤细胞系中血管内皮生长因子和白细胞介素-8 的表达,并消除下游血管生成过程。 | |||
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。 | |||
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。 | |||
T9659 |
LCB 03-0110
3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol |
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
LCB 03-0110 (3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol) 是一种盘状结构域受体家族酪氨酸激酶的强效抑制剂,可强烈抑制多种酪氨酸激酶,包括 c-Src 家族、脾酪氨酸激酶、布鲁顿酪氨酸激酶和血管内皮生长因子受体 2,它们对免疫很重要细胞信号传导和炎症反应。 | |||
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。 | |||
T2500L |
Cediranib maleate
AZD-2171,Recentin,西地尼布马来酸盐,AZD2171,AZD2171 maleate,AZD 2171 |
||
Cediranib is a potent and selective inhibitor of VEGF with antineoplastic activities. It inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth. | |||
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... | |||
T71576 |
SIM010603
|
||
SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Mor... | |||
T71204 |
Apatinib HC
Rivoceranib HCl,YN-968D1 HCl |
||
Apatinib, also known as Rivoceranib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SR... | |||
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... | |||
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. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPJ-00603 |
TL1A/TNFSF15 Protein, Mouse, Recombinant
TNFSF15,Tumor Necrosis Factor Ligand Superfamily Member 15,V... |
Mouse | E. coli |
Tumor Necrosis Factor Ligand Superfamily Member 15 (TNFSF15) is a new member of the tumor necrosis factor family. TNFSF15 is predominantly an endothelial cell-specific gene, and recombinant TNFSF15 is a potent inhibitor of endothelial cell proliferation, angiogenesis and tumor growth. TNFSF15 exerts two activities on endothelial cells: early G1 arrest of G0/G1-cells responding to growth stimuli and programmed cell death of proliferating cells. These activities are highly specific to endothelial ... | |||
TMPY-01484 |
THSD1 Protein, Mouse, Recombinant (His)
4833423O18Rik,thrombospondin type 1 domain containing 1,Tmts... |
Mouse | HEK293 Cells |
Thrombospondin type-1 domain-containing protein 1, also known as transmembrane molecule with thrombospondin module, THSD1 and TMTSP, is a single-pass type I membrane protein that contains one TSP type-1 domain. THSD1 is a multi-domain, multi-functional glycoprotein synthesized by many cells. Matricellular THSD1 modulates cell adhesion and proliferation. It is involved in angiogenesis, inflammation, wound healing and cancer. In vitro, nanomolar concentrations of Thrombospondin-1 are required to a... |