Angiogenesis
Angiogenesis is the formation and remodelling of new blood vessels and capillaries from growth of pre-existing blood vessels. It normally occurs during wound healing and embryonic development, but is also required for tumour growth and metastasis in cancer.
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PDGFRα/β 抑制剂
CP 673451是一种有效的PDGFR-β抑制剂，IC50为1 nM。
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- Kaori Aoto, .et al. Complex formation between platelet-derived growth factor receptor β and transforming growth factor β receptor regulates the differentiation of mesenchymal stem cells into cancer-associated fibroblasts, Oncotarget, 2018, Sep 25; 9(75): 34090-34102 PMID: 30344924
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KIT/PDGFR 抑制剂
Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。
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- Julia M Harrison, .et al. Muscle fiber-type specific terminal Schwann cell pathology leads to sprouting deficits following partial denervation in SOD1 G93A mice, Neurobiol Dis, 2020, Aug 20;145:105052 PMID: 32827689
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c-Kit 抑制剂
Masitinib (AB1010)是一种蛋白质酪氨酸激酶抑制剂。
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PDGFR/FLT3 抑制剂
Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。
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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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VEGFR/PDGFR 抑制剂
Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。
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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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Bcr-Abl 抑制剂
Imatinib mesylate是一种选择性酪氨酸激酶抑制剂，通过抑制KIT信号转导途径，在治疗胃肠间质瘤中诱导了持续的客观反应。
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- Inge Govaerts, .et al. PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia, J Hematol Oncol, 2021, 14: 97 PMID: 34167562
- Genevra Kuziel, .et al. Stromal CCL2 Signaling Promotes Mammary Tumor Fibrosis through Recruitment of Myeloid-Lineage Cells, Cancers (Basel), 2020, Jul 28;12(8):E2083 PMID: 32731354
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VEGFR-2 抑制剂
ki8751是一种细胞可渗透的喹啉氧基苯基脲化合物，在基于细胞和无细胞的检测中起Flk-1 (VEGFR-2)选择性抑制剂的作用。
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- Kohei Ashina, .et al. VEGF-induced blood flow increase causes vascular hyper-permeability in vivo, Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262
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c-Kit, PDGFR, VEGFR 抑制剂
Toceranib (PHA 291639,SU 11654)是一种激酶抑制剂，通过抑制KIT，血管内皮生长因子受体2和PDGFRβ同时具有抗肿瘤和抗血管生成活性。
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- Masaya Igase, .et al. Oncolytic reovirus synergizes with chemotherapeutic agents to promote cell death in canine mammary gland tumor, Can J Vet Res, 2016, Jan; 80(1): 21-31 PMID: 26733729
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M-CSFR, CSF1R 抑制剂
Ki 20227是c-Fms酪氨酸激酶(M-CSFR,CSF1R)的抑制剂。
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- Wensheng Wang, .et al. Lymphatic endothelial cells produce M-CSF causing massive bone loss in mice, J Bone Miner Res, 2017, May; 32(5): 939-950 PMID: 28052488
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂
AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。
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RTK 抑制剂
MP470 (MP-470,Amuvatinib)是c-Kit/PDGFR酪氨酸激酶抑制剂。
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VEGFR-2 抑制剂
Telatinib (BAY 57-9352)是一种口服的血管内皮生长因子受体2和3（VEGFR2/3）和血小板衍生的生长因子受体β酪氨酸激酶的小分子抑制剂，IC50分别为6 nM/4 nM，1 nM和15 nM。
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PI3K 抑制剂
PP121是一种作用于PDGFR，Hck，mTOR，VEGFR2，Src和Abl的多靶点抑制剂，IC50分别为2 nM，8 nM，10 nM，12 nM，14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。
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VEGFR 抑制剂
Motesanib也称为AMG-706，是一种有效的ATP竞争性的VEGFR1/2/3抑制剂，IC50分别为2 nM/3 nM/6 nM；对Kit具有相似的抑制活性，对VEGFR选择性比PDGFR和Ret高10倍。
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VEGFR 抑制剂
KRN 633是一种细胞可渗透、可逆、ATP竞争性VEGFR激酶抑制剂，仅在较高浓度下(IC50 = 0.97 μM和4.33 μM)抑制PDGFR-α和C-Kit，对其他17种激酶无活性(IC50 ≥ 10 μM)。
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c-Abl/c-Kit/PDGRFβ 抑制剂
Flumatinib mesylate以时间和剂量依赖性的方式降低U266细胞中C-MYC，HIF-1a和VEGF的表达，因此甲磺酸氟马替尼可能成为MM治疗的新药。
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mutil-targeted protein tyrosine kinase 抑制剂
AZD2932是一种有效且靶向多用途的蛋白酪氨酸激酶抑制剂，对VEGFR-2，PDGFRβ，Flt-3和c-Kit的IC50分别为8 nM，4 nM，7 nM和9 nM。
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VEGFR2/PDGFRβ/EphB4 抑制剂
JI-101是一种具有血管内皮生长因子受体2（VEGFR2），血小板源性生长因子受体β（PDGFRβ）和ephrin B4受体B4（EphB4）的口服活性抑制剂，具有潜在的抗血管生成和抗肿瘤活性。
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VEGFR/PDGFR 抑制剂
TAK-5933是一种口服制剂，其中含有血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的小分子受体酪氨酸激酶抑制剂，具有潜在的抗肿瘤活性。
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C-Kit/PDGFR 抑制剂
DCC-2618是c-Kit和PDGFR的小分子抑制剂，对c-Kit /PDGFRα/PDGFRβ的IC50分别为6 nM/30 nM/13 nM。
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VEGFR/PDGFRβ/KIT 抑制剂
N-Desethyl Sunitinib是舒尼替尼的主要药理活性代谢产物，是有效的，ATP竞争性VEGFR，PDGFRβ和KIT抑制剂（VEGFR -1，-2，-3的Ki值为2、9、17、8和4 nM。分别为PDGFRβ和KIT）。
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Tyrosine kinase 抑制剂
Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂，IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。
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Toceranib phosphate是通过抑制KIT，血管内皮生长因子受体2和PDGFRβ而具有抗肿瘤和抗血管生成活性的激酶抑制剂。
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂
AC710是一种有效的，具有活性的，选择性血小板衍生的生长因子受体家族激酶抑制剂，具有潜在的抗癌活性。
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multi-kinase 抑制剂
Flumatinib是一种多激酶抑制剂，对c-Abl，PDGFRbeta和c-Kit的IC50值分别为1.2 nM，307.6 nM和2662 nM。
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VEGF and PDGF 抑制剂
Ningetinib Tosylate (CT-053Tosylate,DE-120)是一种VEGF和PDGF抑制剂，可能用于治疗与年龄相关的湿性黄斑变性。CAS：1394820-69-9（游离碱）1394820-77-9（甲苯磺酸酯）
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PDGFR 抑制剂
AG1295 is a PDGF receptor specific inhibitor.
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VEGFR/PDGFR 抑制剂
Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor.
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VEGFR 抑制剂
Vandetanib (ZD6474)是一种VEGFR和EGFR拮抗剂，是一种酪氨酸激酶抑制剂，对于HUVEC增殖，PC-9细胞和酪氨酸激酶活性，IC50为60、90、40 nM。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Shinya Kitamura, .et al. Vandetanib inhibits cell growth in EGFR-expressing cutaneous squamous cell carcinoma, Biochem Biophys Res Commun, 2020, Aug 13 PMID: 32800552
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Rintaro Sogawa, .et al. Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib, JPA, 2018, in Press PMID: 30740257
- Park K, .et al. Vascular endothelial growth factor receptor 1 (VEGFR1) tyrosine kinase signaling facilitates granulation tissue formation with recruitment of VEGFR1+ cells from bone marrow, Anat Sci Int, 2018, Jun;93(3):372-383 PMID: 29256114
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Park K, .et al. Vascular endothelial growth factor receptor-1 (VEGFR-1) signaling enhances angiogenesis in a surgical sponge model, Biomed Pharmacother, 2016, Mar;78:140-149 PMID: 26898435
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VEGFR 抑制剂
SU 5416 (Semaxinib)是血管内皮生长因子受体（VEGFR）的抑制剂，它还抑制其他酪氨酸激酶KIT，MET，FLT3和RET。
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- Guangyan Zhang, .et al. Sulforaphane Does Not Protect Right Ventricular Systolic and Diastolic Functions in Nrf2 Knockout Pulmonary Artery Hypertension Mice, Cardiovasc Drugs Ther, 2022, Feb 14 PMID: 35157168
- Michel R. Corboz, .et al. Treprostinil palmitil inhibits the hemodynamic and histopathological changes in the pulmonary vasculature and heart in an animal model of pulmonary arterial hypertension, Eur J Pharmacol, 2022, 916: 174484 PMID: 34508752
- Avner Adini, .et al. PR1P Stabilizes VEGF and Upregulates its Signaling to Reduce Elastase Induced Murine Emphysema, Am J Respir Cell Mol Biol, 2020, Jul 14 PMID: 32663413
- Yin Kang, .et al. Sulforaphane Prevents Right Ventricular Injury and Reduces Pulmonary Vascular Remodeling in Pulmonary Arterial Hypertension, Am J Physiol Heart Circ Physiol, 2020, Apr 1;318(4):H853-H866 PMID: 32108526
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VEGFR 抑制剂
E7080 (Lenvatinib)是一种多激酶抑制剂，可同时抑制VEGFR2和VEGFR3激酶。
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- Mai Nakahara, .et al. Effect of Lenvatinib treatment on the cell cycle and microRNA profile in hepatocellular carcinoma cells, Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Keisuke Enomoto, .et al. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models, Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. Validation of a Liquid Chromatography-Tandem Mass Spectrometric Assay for Quantitative Analysis of Lenvatinib in Human Plasma, Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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c-MET 抑制剂
Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。
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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166–174. PMID: 25351743
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VEGFR 抑制剂
XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。
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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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VEGFR 抑制剂
Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍 和1000倍以上。
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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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VEGFR-2 抑制剂
Taxifolin以很大的结合能值结合在VEGFR-2激酶的ATP结合位点上，并起I型竞争性抑制剂的作用。
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- Keji Yu, .et al. A role for ascorbate conjugates of (+)-catechin in proanthocyanidin polymerization, Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. Antidiabetic Effect of Taxifolin in Cultured L6 Myotubes and Type 2 Diabetic Model KK-Ay/Ta Mice with Hyperglycemia and Hyperuricemia, Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. Anti-hyperuricemic effect of taxifolin in cultured hepatocytes and model mice, Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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VEGFR 抑制剂
Apatinib (YN968D1)是一种酪氨酸激酶抑制剂，可选择性抑制血管内皮生长因子受体2（VEGFR2，也称为KDR），后者可抑制VEGF介导的内皮细胞迁移和增殖，从而阻止肿瘤组织中新血管的形成。
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- Wonjin Park, .et al. Human plasminogen-derived N-acetyl-Arg-Leu-Tyr-Glu antagonizes VEGFR-2 to prevent blood-retinal barrier breakdown in diabetic mice, Biomed Pharmacother, 2021, Feb;134:111110 PMID: 33338749
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
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(-)-Catechin gallate是绿茶的抗氧化成分。在uM浓度下，抑制VEGF诱导的酪氨酸磷酸化。
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VEGFR 抑制剂
Motesanib(AMG706)是一种多激酶抑制剂，可选择性靶向VEGF受体，血小板衍生的生长因子受体（PDGFRs）和Kit受体，并带有IC50受体。值分别为2 nM（VEGFR1），3 nM（VEGFR2），6 nM（VEGFR3），84 nM（PDGFR）和8 nM（Kit）。
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VEGFR 抑制剂
SU14813 double bond Z是针对血管内皮生长因子受体（VEGFR），血小板源性生长因子受体（PDGFR），Kit和fms样酪氨酸激酶3（FLT-3）的多靶酪氨酸激酶抑制剂（TKI）。
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VEGFR2/Src kinase 抑制剂
TG 100572 HCl是一种多靶点激酶抑制剂，可抑制选择性生长因子受体酪氨酸激酶和Src家族激酶，分别对VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse的IC50值为2/7/2/1/0.5 nM。
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VEGFr2 抑制剂
TG 100801 HCl是TG 100572（HY-10184）的前药，TG 100572是一种多靶点激酶抑制剂，可抑制选择性生长因子受体酪氨酸激酶和Src家族激酶，IC50值为2/7/2/1/0.5 nM或VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse分别。
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VEGFR 抑制剂
Vandetanib hydrochloride是一种有效的VEGFR2抑制剂，IC50为40 nM。
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VEGFR 抑制剂
ZM323881是一种有效且选择性的人血管内皮生长因子受体2（VEGFR-2/KDR）抑制剂，IC50值为2 nM。
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VEGFR 抑制剂
SU10944是VEGFR的小分子激酶抑制剂，可抑制新血管形成和通透性，并在全身递送时分配到眼睛。
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
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VEGFR2 inhibitor
VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.
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VEGFR inhibitor
ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
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VEGFR inhibitor
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
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VEGFR/c-Met/HGFR inhibitor
TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
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VEGFR2/KDR inhibitor
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
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