Platelet-derived growth factor receptors (PDGFRs) belong to the receptor tyrosine kinase (RTK) family and serve the function of protein tyrosine kinases.PDGFRs are involved in a number of cellular processes, such as proliferation, migration, survival, and the emergence of cancer, and they are activated by binding to their ligand, PDGFs. Vascular endothelial cells, fibroblasts, and Kupffer cells are where PDGFRs are primarily found. The two receptor types, PDGFR- and PDGFR-, share structural similarities and are made up of intracellular kinase domains with distinctive inserts of about 100 amino acid residues that have no homology to kinases and extracellular domains with five immunoglobulin (Ig)-like domains.Direct receptor-receptor interactions involving Ig-like domain 4 stabilize the receptor dimerization, which is primarily caused by ligand binding to Ig-like domains 2 and 3.The juxtaposition of the intracellular components during dimerization, which encourages autophosphorylation in trans between the receptors, is a crucial step in activation. The phosphorylated PDGFR then recruits molecules with SH2 domains like Src kinase, Grb2, SHP2, PLC, Nck, and STAT to start various downstream signaling events.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V0578 | Sennoside B | 128-57-4 | Sennoside B is a naturally occuring anthraquinone glycoside compound isolated from Puffer fish, salamanders, frogs foot spot et al. |
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V41775 | Seralutinib (PK-10571; GB-002) | 1619931-27-9 | Seralutinib (PK-10571; GB-002) is a novel and potent PDGFRα/β inhibitor used as an inhaled formulation for the treatment of PAH (pulmonary arterial hypertension). |
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V15397 | SU-4312 | 5812-07-7 | SU-4312, formerly known as DMBI, is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 are 0.8 and 19.4 μM respectively). |
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V29102 | SU14813 maleate | 849643-15-8 | SU14813 maleate is a novel, orally bioavailable, multi-targeted tyrosine kinase inhibitor (TKI) with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT, respectively. |
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V4585 | TAK-593 | 1005780-62-0 | TAK-593 is a novel, orally bioavailable and potent small-molecule receptor of VEGFR and PDGFR with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively. |
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V3698 | Toceranib | 356068-94-5 | Toceranib (formerly known as PHA-291639, or SU-11654) is an inhibitor of receptor tyrosine kinase (RTK) with anticancer activities. |
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V3699 | Toceranib phosphate | 874819-74-6 | Toceranib phosphate (formerly known as PHA291639; SU11654),phosphate salt ofToceranib,is a novel and potent receptor tyrosine kinase (RTK)inhibitor with antineoplastic/anticancer activities. |
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V69297 | Toceranib-d8 (Toceranib d8) | 1795134-78-9 | Toceranib-d8 is the deuterated form of Toceranib. |
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V69538 | Tovetumab (MEDI-575) | 1243266-04-7 | Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody (mAb) that selectively blocks PDGFRα signaling. |
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V15474 | Trapidil (AR12008) | 15421-84-8 | Trapidil is a vasodilator, an antiplatelet active molecule with specificity for platelet-derived growth factor. |
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V0574 | Tyrphostin AG 1296 | 146535-11-7 | Tyrphostin AG 1296 (AG-1296) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR with potential antitumor activity. |
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