目录号 | 产品详情 | 靶点 | |
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T8402 | Raf VEGFR c-RET PDGFR Autophagy | ||
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) 是一种新型口服多激酶抑制剂,可抑制血管生成、基质和致癌受体酪氨酸激酶,具有强大的临床前抗肿瘤活性。它靶向作用于 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1,IC50值分别为 13/4.2/46、22、7、1.5 和 2.5 nM。 | |||
TQ0059 | VEGFR FLT c-RET PDGFR Aurora Kinase | ||
Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂,可抑制 Aurora A、Aurora B 和Aurora C,IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1,IC50为7 nM、3 nM 和 32 nM。 | |||
T74000 | VEGFR | ||
CP-547632 TFA是一款口服效果显著的ATP競爭性抑制劑,针对VEGFR-2和FGF激酶具有高度选择性,IC50值分别为11 nM和9 nM。该化合物相较于EGFR和PDGFRβ,对VEGFR2和bFGF展现出更高的选择性,优于相关的酪氨酸激酶(TKs)。CP-547632 TFA还显示了显著的抗肿瘤活性。 | |||
T75163 | VEGFR CDK Src | ||
GW297361 是一种有效的依赖细胞周期蛋白的激酶 Cdk1 抑制剂,对 Pho85 信号通路也具有抑制作用。GW297361对酵母 Cdk1 和 Pho85 的 IC50 分别为 20 nM 和 400 nM。 | |||
T14943 | VEGFR CDK PKC | ||
CGP60474 是一种高效的抗内毒素药物,抑制细胞周期蛋白依赖激酶(CDK) ,抑制 CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC 抑制剂。 | |||
T83911 | |||
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 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 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D...... | |||
T71082 | |||
DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.) | |||
T11638 | Aurora Kinase | ||
Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1 nM, 7 nM, 120 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM). | |||
T83680 | |||
Azurin (50-77)是一种含铜细菌蛋白azurin的肽段,存在于P. aeruginosa中,具有细胞周期停滞、抑制癌细胞增殖和调节血管生成活性。作为VEGFR2的抑制剂(IC20约为10.7 µM),Azurin (50-77)(20 µM)能在MCF-7乳腺癌细胞中诱导G2/M期的细胞周期停滞。在50 µM的浓度下,减少MCF-7和ZR-75-1乳腺癌细胞的增殖。Azurin (50-77)以25 µM的浓度减少VEGF-A诱导的毛细管管腔形成(IC50 = 12 µM),降低人脐静脉内皮细胞(HUVECs)中与细胞膜相关的F-actin、焦点粘附激酶(FAK)和paxillin的水平,并增加胞外的血小板内皮细胞粘附分子-1(PECAM-1)的水平。在体内,Azurin (50-77)(每日10 mg/kg)在MCF-7小鼠异种移植模型中减少肿瘤体积。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02361 | VEGFR2/KDR Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.6 kDa and the accession number is P35968-1.
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TMPY-01044 | VEGFR2/KDR Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 109 kDa and the accession number is P35968-1.
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TMPY-05657 | VEGFR2/KDR Protein, Human, Recombinant (hFc), Biotinylated | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (hFc), Biotinylated is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 61.5 kDa and the accession number is P35968-1.
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TMPY-04940 | VEGFR2/KDR Protein, Human, Recombinant (His), Biotinylated | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (His), Biotinylated is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.6 kDa and the accession number is P35968-1.
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TMPY-04530 | VEGFR2/KDR Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 89.3 kDa and the accession number is P35968-1.
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TMPY-02736 | VEGFR2/KDR Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
VEGFR2/KDR Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.5 kDa and the accession number is P35918-1.
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TMPY-05610 | VEGFR2/KDR Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with His and Avi tag. The predicted molecular weight is 86.5 kDa and the accession number is P35968-1.
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TMPK-00645 | VEGFR2/KDR Protein, Rhesus macaque, Recombinant (His) | Rhesus | HEK293 Cells | ||
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. The tyrosine kinase receptor vascular endothelial growth factor receptor 2 (VEGFR2) is a key regulator of angiogenesis. VEGFR2/KDR Protein, Rhesus macaque, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 84.37 kDa and the accession number is F7E313.
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TMPK-00454 | VEGFR2/KDR Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. The tyrosine kinase receptor vascular endothelial growth factor receptor 2 (VEGFR2) is a key regulator of angiogenesis. VEGFR2/KDR Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 86.2 kDa and the accession number is P35968-1.
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TMPY-04802 | VEGFR2/KDR Protein, Human, Recombinant (Domain 2&3, hFc) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (Domain 2&3, hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 50.4 kDa and the accession number is P35968-1.
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TMPY-04796 | VEGFR2/KDR Protein, Human, Recombinant (Domain 2&3, His) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (Domain 2&3, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 24.8 kDa and the accession number is P35968-1.
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TMPY-04794 | VEGFR2/KDR Protein, Human, Recombinant (Domain 1&2&3, hFc) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (Domain 1&2&3, hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 61.5 kDa and the accession number is P35968-1.
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TMPY-04795 | VEGFR2/KDR Protein, Human, Recombinant (Domain 1&2&3, His) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (Domain 1&2&3, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 35.9 kDa and the accession number is P35968-1.
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TMPY-02858 | VEGFR2/KDR Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
VEGFR2/KDR Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 110 kDa and the accession number is P35918.
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TMPY-04924 | VEGFR2/KDR Protein, Mouse, Recombinant (His), Biotinylated | Mouse | HEK293 Cells | ||
VEGFR2/KDR Protein, Mouse, Recombinant (His), Biotinylated is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.5 kDa and the accession number is P35918-1.
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TMPJ-00593 | VEGFR2/KDR Protein, Human, Recombinant (aa 20-764, His) | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (aa 20-764, His) is expressed in HEK293 mammalian cells with C-6xHis tag. The predicted molecular weight is 110-140 KDa and the accession number is AAI31823.1.
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TMPJ-00414 | VEGFR2/KDR Protein, Human, Recombinant (aa 20-764, His & Avi), Biotinylated | Human | HEK293 Cells | ||
VEGFR2/KDR Protein, Human, Recombinant (aa 20-764, His & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-6xHis-Avi tag. The predicted molecular weight is 120-150 KDa and the accession number is P35968.
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TMPY-03202 | VEGFR2/KDR Protein, Rat, Recombinant (hFc) | Rat | HEK293 Cells | ||
VEGFR2/KDR Protein, Rat, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 110 kDa and the accession number is Q5PQU0.
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TMPY-02678 | VEGFR2/KDR Protein, Rat, Recombinant (His) | Rat | HEK293 Cells | ||
VEGFR2/KDR Protein, Rat, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.3 kDa and the accession number is A6HDB7.
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TMPY-05382 | VEGFR2/KDR Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
VEGFR2/KDR Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 84.7 kDa and the accession number is G7P5T2.
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TMPJ-00864 | VEGF165 Protein, Human, Recombinant | Human | HEK293 Cells | ||
Human Vascular endothelial growth factor (VEGF), also known as VEGF-A and vascular permeability factor (VPF), belongs to the platelet-derived growth factor family of cysteine-knot growth factors. It is a potent activator in vasculogenesis and angiogenesis both physiologically and pathologically. VEGF-A has 8 differently spliced isoforms, of which VEGF165 is the most abundant one. VEGF165 is a disulfide-linked homodimer consisting of two glycosylated 165 amino acid polypeptide chains. VEGF stimulates the cellular response through binding to tyrosine kinase receptors VEGFR1 and VEGFR2 on the cell surface. It is widely accepted that VEGFR2 mediate almost all of the known cellular responses to VEGF while the function of VEGFR1 is less defined and is thought to modulate the VEGFR2 signaling.
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TMPJ-00865 | VEGF121 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Human VEGF121, also known as Vascular endothelial growth factor A, VEGFA, Vascular permeability factor, VPF and VEGF, is a homodimeric, heparin-binding glycoprotein which belongs to the platelet-derived growth factor (PDGF)/vascular endothelial growth factor (VEGF) family. VEGF-A is a glycosylated mitogen that specifically acts on endothelial cells and has various effects, including mediating increased vascular permeability, inducing angiogenesis, vasculogenesis, permeabilization of blood vessels and endothelial cell growth, increasing microvascular permeability, promoting cell migration and inhibiting apoptosis. Alternatively spliced transcript variants of VEGF-A encod either secreted or cell-associated isoforms. The lymphangiogenesis may be promoted by upregulation of VEGF121, which may in turn act in part via induction of VEGF-C. It binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activate downstream signaling pathways, does not activate angiogenesis and inhibits tumor growth.
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TMPH-01201 | DRD2 Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5.
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TMPK-00489 | TL1A/TNFSF15 Protein, Cynomolgus/Rhesus macaque, Recombinant (His) | Cynomolgus,Rhesus | HEK293 Cells | ||
TNF superfamily member 15 (TNFSF15), a cytokine largely produced by vascular endothelial cells and a specific inhibitor of the proliferation of these same cells, can inhibit VEGF-induced vascular permeability in vitro and in vivo, and that death receptor 3 (DR3), a cell surface receptor of TNFSF15, mediates TNFSF15-induced dephosphorylation of VEGFR2. TNFSF15 Protein, Cynomolgus/Rhesus macaque, Recombinant (His) is expressed in HEK293 mammalian cells with N-His tag. The predicted molecular weight is 21.52 kDa and the accession number is A0A2K5UA22.
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TMPK-00143 | TL1A/TNFSF15 Trimer Protein, Human, Recombinant (His & Flag) | Human | HEK293 Cells | ||
TNF superfamily member 15 (TNFSF15), a cytokine largely produced by vascular endothelial cells and a specific inhibitor of the proliferation of these same cells, can inhibit VEGF-induced vascular permeability in vitro and in vivo, and that death receptor 3 (DR3), a cell surface receptor of TNFSF15, mediates TNFSF15-induced dephosphorylation of VEGFR2. TNFSF15 Trimer Protein, Human, Recombinant (His & Flag) is expressed in HEK293 mammalian cells with N-His-Flag tag. The predicted molecular weight is 58.2 kDa and the accession number is O95150-1.
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