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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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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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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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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VEGFR 抑制剂
Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。
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- Youcef M. Rustum, .et al. Non-Coding Micro RNAs and Hypoxia-Inducible Factors Are Selenium Targets for Development of a Mechanism-Based Combination Strategy in Clear-Cell Renal Cell Carcinoma-Bench-to-Bedside Therapy, Int J Mol Sci, 2018, Nov; 19(11): 3378 PMID: 30380599
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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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RTK inhibitor
Sunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，也会抑制c-Kit的活性。用于治疗肾细胞癌（RCC）和伊马替尼耐药的胃肠道间质瘤（GIST）。
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- Rachel K Toth, .et al. Stabilization of PIM Kinases in Hypoxia Is Mediated by the Deubiquitinase USP28, Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- 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
- 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
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PDGFR 抑制剂
Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂，抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6，0.1和0.1 μM。
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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
- Takafumi Shima, .et al. Glucose transporter-1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells, Oncol Rep, 2022, 47: 7 PMID: 34738628
- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BM Duggan, .et al. RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice, Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- 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
- 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
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VEGFR 抑制剂
Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。
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- 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
- 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
- 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
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- 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
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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VEGFR 抑制剂
Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。
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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
- 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
- Majid Momeny, .et al. Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells, Sci Rep, 2017, 7: 44075 PMID: 28287096
- Nicholas A. Manieri, .et al. Mucosally transplanted mesenchymal stem cells stimulate intestinal healing by promoting angiogenesis, J Clin Invest, 2015, Sep 1; 125(9): 3606-3618 PMID: 26280574
- Usui T, .et al. Brain-derived neurotrophic factor promotes angiogenic tube formation through generation of oxidative stress in human vascular endothelial cells., Acta Physiol (Oxf), 2014, 211, 385-394 PMID: 24612679
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Raf 抑制剂
Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。
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- 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
- 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
- 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
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- 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
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- 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
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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VEGFR 抑制剂
Brivanib alaninate (BMS-582664)是VEGFR和FGFR信号转导的双重酪氨酸激酶抑制剂。
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。
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RTK 抑制剂
Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。
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c-Met 抑制剂
MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。
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FGFR/VEGFR2 抑制剂
LY2874455是一种新型有效的FGFR / VEGFR抑制剂。
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂
R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。
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FGFR1 抑制剂
SSR128129E是一种口服活性变构FGFR1抑制剂，IC50为1.9 uM。
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FGFR1/2/3 抑制剂
Debio-1347 (CH5183284)是成纤维细胞生长因子受体亚型1（FGFR-1），2（FGFR-2）和3（FGFR-3）的生物利用抑制剂，具有潜在的抗肿瘤活性。
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FGFR1 抑制剂
ACTB-1003是一种口服激酶抑制剂，靶向癌症突变（FGFR抑制），血管生成（抑制VEGFR2和Tie-2）并诱导凋亡（靶向PI3激酶下游的RSK和p70S6K。
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VEGFR/FGFR 抑制剂
E-3810是一种有效且选择性的VEGF和FGF受体双重抑制剂，对VEGFR-1，VEGFR-2，VEGFR-3，FGFR-1和VEGF的IC50值分别为7nM，25nM，10nM，17.5nM和82.5nM。FGFR-2。
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FGFR 抑制剂
NVP-BGJ398 phosphate是一种新型的选择性泛特异性FGFR抑制剂，对FGFR1，FGFR2和FGFR3的IC50分别为0.9、1.4和1 nM。与FGFR4和VEGFR2相比，对FGFR具有40倍以上的选择性，并且对Abl，Fyn，Kit，Lck，Lyn和Yes的活性很小。
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FGFR 抑制剂
BLU9931是第一种选择性的FGFR4小分子抑制剂，IC50为3 nM。对FGFR1/2/3的效力较低（IC50> 150 nM）。
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FGFR 抑制剂
FIIN-2是FGFR1-4的不可逆抑制剂，IC50值分别为3.1、4.3、27和45 nM。
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FGFR2 抑制剂
Alofanib (RPT835)是FGFR2的强效选择性变构抑制剂，具有潜在的抗癌活性。
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FGFR 抑制剂
Erdafitinib (JNJ-42756493)是一种有效且选择性的口服生物利用型泛成纤维细胞生长因子受体（FGFR）抑制剂，具有潜在的抗肿瘤活性。
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FGFR4 抑制剂
FGFR4-IN-1是有效的FGFR4抑制剂，IC50为0.7 nM。
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