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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V2880 | AC710 | 1351522-04-7 | AC710 is a potent, orally bioactive, and selectiveinhibitor of PDGFR (platelet-derived growth factor receptor) family kinase withKdvalues of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively. |
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V2093 | AC710 Mesylate | 1351522-05-8 | AC710 mesylate, the mesylate salt of AC710, is a potent, orally bioactive, and selectiveinhibitor of PDGFR (platelet-derived growth factor receptor) family kinase withKdvalues of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively. |
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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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V3285 | Anlotinib | 1058156-90-3 | 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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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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V0577 | CP-673451 | 343787-29-1 | CP-673451 (CP673451) is a novel, potent, selective and ATP-competitive inhibitor of PDGFR(α/β) with potential antitumor activity. |
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V0580 | Crenolanib (CP-868596; RO 002; ARO 002) | 670220-88-9 | Crenolanib (formerly also known as CP868596; RO-002; ARO-002), a benzimidazole compound, is an orally bioavailable and selective small molecule inhibitor of platelet-derived growth factor receptor (PDGFRα/β) with potential anticancer activity. |
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V79582 | Gint4.T aptamer sodium | Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). | |
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V0573 | Imatinib (STI571; Gleevec; Glivec) | 152459-95-5 | Imatinib (formerly STI-571, trade name Gleevec and Glivec) is an orally bioavailable multi-targeted kinase inhibitor with potential anticancer activity. |
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V25190 | INVIVO74978 | 778274-97-8 | multikinase inhibitor 1 is a potent multikinase inhibitor. |
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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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V0575 | MK-2461 | 917879-39-1 | MK-2461 (MK2461) is a novel,potent, ATP-competitive, multi-targeted inhibitor for c-Met (WT/mutants) with potential antineoplastic activity. |
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V69534 | N-(p-Coumaroyl) Serotonin | 68573-24-0 | N-(p-Coumaroyl) Serotonin is a polyphenol extracted from safflower seeds that displays antioxidant, antiatherogenic, and anti-inflammatory activities. |
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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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V69531 | Olaratumab (IMC-3G3; LY3012207) | 1024603-93-7 | Olaratumab (IMC-3G3; LY3012207) is a human monoclonal IgG1 antibody against platelet-derived growth factor receptor alpha (PDGFRα) with anti-tumor activity. |
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V13080 | PDGF Receptor Tyrosine Kinase Inhibitor III | 205254-94-0 | PDGF Receptor Tyrosine Kinase Inhibitor III (also known as PDGFR Tyrosine Kinase Inhibitor III) is a novel and potent PDGFR inhibitor. |
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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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V69536 | Rinucumab (REGN 2176) | 1569263-06-4 | Rinucumab (REGN 2176) is a monoclonal antibody (mAb) that is an inhibitor (blocker/antagonist) of PDGF. |
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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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