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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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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V3285 | Anlotinib | 1058156-90-3 | This product is discontinued due to commercial reason.Anlotinib (formerlyknown as AL3818) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3,FGFR1-4,PDGFRα/β,c-Kit, andRet. |
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V10056 | Nintedanib esylate | 656247-18-6 | Nintedanib esylate (formerly also known as BIBF 1120 esylate; BIBF-1120 esylate;Vargatef), theesylate salt of nintedanib, is a novel, orally bioavailable, potent triple angiokinase inhibitor that has gained FDA approval in 2014 for the treatment of idiopathic pulmonary fibrosis (IPF). |
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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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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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V29157 | Regorafénib N-oxyde (M2) | 835621-11-9 | Regorafénib N-oxyde M2 is a major and active metabolite of Regorafenib. |
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V3284 | Ripretinib (DCC-2618) | 1442472-39-0 | Ripretinib (DCC-2618; DCC2618; Qinlock) is a potent, orally bioactive, and spectrum-selective pan KIT and PDGFRA inhibitor approved in 2020 as an anticancer medication for treating gastrointestinal stromalcancers. |
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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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V3286 | Anlotinib Dihydrochloride | 1360460-82-7 | Anlotinib Dihydrochloride (formerlyknown as AL3818 Dihydrochloride) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3,FGFR1-4,PDGFRα/β,c-Kit, andRet. |
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V0579 | Amuvatinib (MP470; HPK56) | 850879-09-3 | Amuvatinib (MP-470; HPK-56) is a novel, potent, orally bioavailableand multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with potential antineoplastic activity. |
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V0576 | Masitinib (AB1010) | 790299-79-5 | Masitinib (formerly also known as AB1010) is a novel, potent, orally bioavailable, selective and multi-targeted inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, it shows weak inhibition to ABL and c-Fms. |
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V29483 | Methylnissolin | 73340-41-7 | Methylnissolin, also known as Astrapterocarpan, isolated from Astragalus membranaceus, is a novel and potent bioactive compound. |
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