Tyrosine Kinase - Selective
Receptor tyrosine kinases bind to extracellular ligands/growth factors, which promotes receptor dimerization and autophosphorylation of receptor tyrosine residues. This triggers a cascade of downstream events through phosphorylation of intracellular proteins that ultimately transduce the extracellular signal to the nucleus, causing changes in gene expression. Receptor tyrosine kinases include EGFR/ErbB, PDGFR, VEGFR, FGFR and MET subfamilies etc. Dysfunctions in tyrosine phosphorylation are linked to oncogenic transformation. In additions, various adaptor and effector proteins couple to carboxy-terminal of an active kinase. For instance, binding of the GRB2 adaptor protein activates EGFR and MAPK/ERK signaling.
Non-receptor tyrosine kinases involve many well-defined proteins (e.g. the Src family kinases, c-Abl, and Jak kinases) and other kinases which regulates cell growth and differentiation. For example, Src family kinases are curial for activating and inhibitory pathways in the innate immune response.
- A8706 BLU9931Target: FGFRSummary: 有效的FGFR4不可逆抑制剂
- C3342 MAZ51Target: VEGFRSummary: VEGFR3拮抗剂
- B6176 LOXO-101中文名: 硫酸盐拉罗替尼Target: tropomyosin receptor kinaseSummary: 原肌球蛋白受体激酶(TRK)抑制剂
- B5940 TP-0903中文名: 度博替尼Target: AXLSummary: AXL受体酪氨酸激酶抑制剂,抗癌药
- B5889 EGF8162 Citation中文名: 那扎替尼Target: EGFRSummary: EGFR突变选择性抑制剂
- B5859 Entrectinib中文名: 恩曲替尼Target: Trk Receptors|ALK|ROS1Summary: ALK激酶抑制剂
- B5854 Pexidartinib (PLX3397)3 Citation中文名: 培西达替尼Target: FLT3|c-Kit|CSF1RSummary: CSF-1R抑制剂
- B5835 AZD2932Target: FLT3|VEGFR|PDGFR|c-KitSummary: VEGFR-2\PDGFRβ\Flt-3和c-Kit的抑制剂
- B5832 Altiratinib1 CitationTarget: FLT3|VEGFR|Trk Receptors|c-MET|Tie-2Summary: c-MET/TIE-2/VEGFR抑制剂
- B4904 ACTB-1003Target: VEGFR|FGFR|Tie-2|RSK|p70 S6KSummary: FGFR1抑制剂