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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V88059 | cis-SU4312 | 90828-16-3 | cis-SU4312 ((Z)-SU4312) inhibits PDGFR and FLK-1 with IC50 of 19.4 and 0.8 μM, respectively. |
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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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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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V25190 | INVIVO74978 | 778274-97-8 | multikinase inhibitor 1 is a potent multikinase inhibitor. |
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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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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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V88058 | PDGFRα/β/VEGFR-2-IN-1 | PDGFRα/β/VEGFR-2-IN-1 (6f) is a multiple PDGFRα/β and VEGFR-2 tyrosine kinase inhibitor that specifically targets PDGFRα, PDGFRβ, and VEGFR-2 kinases at nanomolar concentrations. | |
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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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V69297 | Toceranib-d8 (Toceranib d8) | 1795134-78-9 | Toceranib-d8 is the deuterated form of Toceranib. |
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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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V96911 | WQ-C-401 | 2376694-72-1 | WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. |
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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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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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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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