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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BCR-ABL 抑制剂
AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。
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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
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- 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
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- 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
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Aurora 抑制剂
Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力 对Lck，VEGFR2/3，c-Kit，CDK2等有效。
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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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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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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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EphB4 抑制剂
NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。
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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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