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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Aurora A/B Kinase 抑制剂
PF-03814735是一种新颖,有效且可逆的Aurora A/B抑制剂,IC50为0.8 nM/5 nM,对Flt3,FAK,TrkA的效力较低,对Met和FGFR1的活性最低。
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PYK2/FAK 抑制剂
PF-4618433与原型BIRB796相比,PF-4618433显示出PYK2效价提高、p38活性降低和总体选择性优越。
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FAK 抑制剂
PF-00562271是PF-562271的苯磺酸盐,是一种有效的,ATP竞争性,可逆的FAK和Pyk2抑制剂,IC50分别为1.5 nM和14 nM。
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FAK/PYK2 抑制剂
PF 431396是一种双粘着斑激酶(FAK)和富含脯氨酸的酪氨酸激酶2(PYK2)抑制剂(IC50值分别为2和11 nM)。
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FAK 抑制剂
PND-1186是一种强效fak抑制剂,ic50为1.5 nm。
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FAK 抑制剂
NVP-TAE 226是一种强效FAK抑制剂,IC50为5.5 nM,对pyk2(IC50=3.5 nM)有适度的强效作用;对InsR, IGF-1R, ALK和c-Met的效力降低10-100倍。
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FAK 抑制剂
PF-04554878 (Defactinib)是一种新型FAK激酶抑制剂,可降低胰腺神经内分泌肿瘤细胞的生长并诱导其凋亡。
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- Shalana O'Brien, .et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics, Oncotarget., 2014, Sep; 5(17): 7945-7959. PMID: 25277206
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FAK 抑制剂
PF-562271是一种有效的,ATP竞争性的,可逆的FAK抑制剂,作用于FAK比作用于Pyk2选择性高10倍左右,比作用于其他蛋白激酶(除了一些CDKs)选择性高100倍以上。
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- Jiping Yue, .et al. In vivo epidermal migration requires focal adhesion targeting of ACF7, Nat Commun, 2016, 7: 11692 PMID: 27216888
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FAK 抑制剂
PF 573228是一种有效和选择性的粘着斑激酶(FAK)抑制剂(IC50 = 4 nM)。
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- Izumi D, .et al. CXCL12/CXCR4 activation by cancer-associated fibroblasts promotes integrin β1 clustering and invasiveness in gastric cancer, Int J Cancer, 2016, Mar 1;138(5):1207-19 PMID: 26414794
- Aya Yokota-Nakatsuma, .et al. Beta 1-integrin ligation and TLR ligation enhance GM-CSF-induced ALDH1A2 expression in dendritic cells, but differentially regulate their anti-inflammatory properties, Sci Rep, 2016, 6: 37914 PMID: 27897208
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FAK/ALK 抑制剂
CEP-37440是一种新型的高效选择性FAK/ALK双重抑制剂,IC50为2.3 nM(FAK)和120 nM(ALK细胞在50%人血浆中的IC50。
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