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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FGFR 抑制剂
BGJ398 (NVP-BGJ398)是一种有效的选择性抑制剂，具有成纤维细胞生长因子受体（FGFR）酪氨酸激酶1、2、3和4的潜在抗血管生成和抗肿瘤活性（对于FGFR1，FGFR2，FGFR3，IC50值为0.9、1.4、1.0和60 nM， 和FGFR4）。
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- Takehito Yamamoto, .et al. Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy, Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- 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
- Anil Kumar, .et al. Human Sertoli cells support high levels of Zika virus replication and persistence, Sci Rep, 2018, 8: 5477 PMID: 29615760
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FGFR 抑制剂
AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。
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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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RTK 抑制剂
Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。
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- 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
- 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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Irreversible FGFR 抑制剂
FIIN-3是一种有效的，选择性的，不可逆的下一代共价FGFR抑制剂。
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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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FGFR/VEGFR2 抑制剂
LY2874455是一种新型有效的FGFR / VEGFR抑制剂。
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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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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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FGFR4 抑制剂
H3B-6527是一种高度选择性的FGFR4抑制剂，在FGF19扩增的细胞系和小鼠中具有强大的抗肿瘤活性。
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