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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RAF/VEGFR 抑制剂
Raf265 derivative是Raf265的衍生物，Raf265是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，IC50为5至10μM。
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c-Kit/VEGFR 抑制剂
OSI-930是Kit，KDR，Flt，CSF-1R，c-Raf和Lck的有效抑制剂，IC50分别为80 nM，9 nM，8 nM，15 nM，41 nM和22 nM。
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Aurora Kinase 抑制剂
CYC116 (CYC-116)是一种有效的Aurora A/B抑制剂，Ki为8.0 nM/9.2 nM，对VEGFR2(Ki为44 nM)作用稍弱。
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VEGFR 拮抗剂
Buflomedil HCl是一种用于治疗外周血管疾病的血管活性剂。
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VEGFR 抑制剂
ZM 323881 hydrochloride是一种有效且选择性的人血管内皮生长因子受体2（VEGFR2/KDR）激酶活性抑制剂。
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VEGFR 抑制剂
ZM 306416 hydrochloride是一种VEGF受体酪氨酸激酶抑制剂，可抑制KDR（IC50 = 100 nM）和Flt（IC50 = 2 uM）酪氨酸激酶。
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E-7050 (Golvatinib)是具有潜在抗肿瘤活性的c-Met(肝细胞生长因子受体)和VEGFR-2(血管内皮生长因子受体-2)酪氨酸激酶的口服生物可利用双重激酶抑制剂。
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VEGFR2 抑制剂
CP-547632是一种新型有效的血管内皮生长因子受体2酪氨酸激酶抑制剂。
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VEGFR 抑制剂
SU14813是一种口服多靶向酪氨酸激酶抑制剂(TKI)，靶向血管内皮生长因子受体(VEGFR)、血小板衍生生长因子受体(PDGFR)、KIT和fms样酪氨酸激酶3 (FLT-3)，抑制 VEGFR2，VEGFR1，PDGFRβ and KIT 的 IC50 值分别为50，2，4，15 nM。
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VEGFR 抑制剂
SKLB1002是一种新型的有效VEGFR2抑制剂，可显着抑制HUVEC增殖，迁移，侵袭和管形成。
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VEGFR2/Src 抑制剂
TG 100572是VEGFR2和Src激酶抑制剂。
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VEGFR2/Src 抑制剂
TG 100801是目前正在临床试验中的靶向VEGFR2的前药。有效形式为TG100572。
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VEGFR3 抑制剂
SAR131675是一种有效的选择性VEGFR-3-TK抑制剂，具有抗淋巴显形、抗肿瘤和抗转移活性。
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VEGFR 抑制剂
SKLB610是一种新型的血管内皮生长因子受体酪氨酸激酶抑制剂，在体内具有抑制血管生成和肿瘤生长的作用。
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VEGFR 抑制剂
Fruquintinib是一种可获得的血管内皮生长因子受体（VEGFR）的小分子抑制剂，具有潜在的抗血管生成和抗肿瘤活性。
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MET/VEGFR-2 抑制剂
BMS-817378是Met/VEGFR-2双重抑制剂BMS-794833的新型前药。
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c-Met/VEGFR 抑制剂
Altiratinib (DCC2701)是一种新型的c-MET/TIE-2/VEGFR抑制剂；与体外HGF拮抗剂相比，可有效降低体内的肿瘤负荷并阻断c-MET pTyr（1349）介导的信号传导，细胞生长和迁移。
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VEGFR-2 抑制剂
NVP-ACC789是VEGFR-2（FLK-1/KDR）的抑制剂。
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VEGFR 抑制剂
NVP-BAW2881是有效的选择性VEGFR抑制剂（血管内皮生长因子受体酪氨酸激酶抑制剂），IC50 为值9 nM，具有抑制慢性和急性皮肤炎症的作用。
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neuropilin-1/VEGF-A 抑制剂
EG00229是第一个对Neuropilin-1和VEGF-A相互作用的小分子抑制剂，IC50抑制8 uM（125I-VEGF与PAE/NRP1细胞结合）。
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VEGFR2 抑制剂
BFH772是一种有效的口服VEGFR2抑制剂，在靶向VEGFR2激酶方面非常有效，IC50值为3 nM。
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VEGFR2 Kinase 抑制剂
SU-5408，也称为VEGFR2激酶抑制剂I，是一种有效的，细胞渗透性的小鼠VEGFR2激酶抑制剂，IC50值为70 nM。
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VEGFR2 抑制剂
SU 5205是VEGFR2抑制剂， IC50 = 9.6 ?M。
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VEGFR-2 抑制剂
Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
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Axl/VEGFR2 抑制剂
R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
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VEGFR2 inhibitor
SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM.
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VEGFR inhibitor
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
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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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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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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
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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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
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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RTK 抑制剂
MP470 (MP-470,Amuvatinib)是c-Kit/PDGFR酪氨酸激酶抑制剂。
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