PDGFR
PDGFR (platelet-derived growth factor receptor) is a receptor tyrosine kinase family that mediates cellular responses to platelet-derived growth factors and regulates proliferation, survival, migration, and tissue development through ligand-induced receptor dimerization and autophosphorylation mechanisms[1][2]. Mechanistically, activated PDGFR recruits multiple signaling mediators, including PI3K, PLCγ, Src-family kinases, and STAT-associated pathways, thereby coordinating cell growth, differentiation, and motility programs that are essential for normal tissue homeostasis and repair[1][2]. In developmental and physiological contexts, PDGFR signaling contributes to organogenesis, mesenchymal cell function, vascular development, and tissue regeneration, highlighting its central role in multicellular tissue organization[2][3]. In disease settings, dysregulated PDGFR activity, including constitutive receptor activation and excessive ligand-driven signaling, has been associated with malignancies, gastrointestinal stromal tumors, chronic eosinophilic leukemia, and other pathological proliferative processes[1][4]. Compared with the related isoforms, PDGFRα binds PDGF-A, PDGF-B, and PDGF-C ligands, whereas PDGFRβ preferentially binds PDGF-B and PDGF-D, resulting in overlapping but biologically distinct signaling capacities and cellular responses[1]. Furthermore, PDGFRβ displays strong chemotactic signaling activity, while PDGFRα can exert different context-dependent effects on cell migration, providing a useful framework for isoform-specific experimental design[1]. For research applications, small-molecule tyrosine kinase inhibitors targeting PDGFR signaling are widely used to investigate receptor-dependent mechanisms and disease-associated signaling networks[3].
References:
- [1]. Huber M. Activation/Inhibition of mast cells by supra-optimal antigen concentrations. Cell Commun Signal. 2013 Jan 22;11(1):7. doi: 10.1186/1478-811X-11-7. PMID: 23339289; PMCID: PMC3598417. et al. Activation/Inhibition of mast cells by supra-optimal antigen concentrations. Cell Commun Signal. 2013 Jan 22;11(1):7. [Content Brief]
- [2]. Andrae J, et al. Role of platelet-derived growth factors in physiology and medicine. Genes Dev. 2008 May 15;22(10):1276-312. [Content Brief]
- [3]. Kanaan R, et al. Use of multitarget tyrosine kinase inhibitors to attenuate platelet-derived growth factor signalling in lung disease. Eur Respir Rev. 2017 Oct 25;26(146):170061. [Content Brief]
- [4]. National Library of Medicine.
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PDGFR Related Products (186)
Related Products (186)
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Pdgfrb Mouse Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS10258Pdgfrb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pdgfrb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Trapidil (Standard)
0 ImagesCat. No.: HY-B1016RCAS No.: 15421-84-8Synonyms: AR-12008 (Standard)Trapidil (Standard) (AR-12008 (Standard)) is the analytical standard of Trapidil (HY-B1016R). This product is intended for research and analytical applications. Trapidil (AR-12008) is an orally active vasodilator and antiplatelet agent. Trapidil antagonizes platelet-derived growth factor (PDGF), inhibits phosphodiesterase, thromboxane A2 synthesis and pro-inflammatory cytokine production. Trapidil promotes prostacyclin biosynthesis, reduces lipid peroxidation, regulates nitric oxide metabolism, and inhibits cell proliferation and migration. Trapidil exerts tissue-protective effects, regulates bone turnover, and inhibits pyroptosis via the GPX3/Nrf2 pathway. Trapidil is applicable to research related to renal ischemia-reperfusion injury, chronic stable angina, restenosis, meningioma, diabetic cardiomyopathy and peripheral nerve crush injury.
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Pimicotinib hydrochloride
0 ImagesCat. No.: HY-153920ACAS No.: 2866305-19-1Synonyms: ABSK021 hydrochloridePimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC50 value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity.
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AK177
0 ImagesCat. No.: HY-181886AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively. AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity.
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Regorafenib monohydrate (Standard)
0 ImagesSynonyms: BAY 73-4506 monohydrate (Standard)Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
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AXL/Angiokinase-IN-1
0 ImagesCat. No.: HY-170776AXL/Angiokinase-IN-1 (compound 11b) is an AXL/triple angiokinase inhibitor, IC50=3.75 nM (AXL expression). AXL/Angiokinase-IN-1 inhibits epithelial-mesenchymal transition (EMT) in Bxpc-3, blocking lung cancer cell metastasis. AXL/Angiokinase-IN-1 also inhibits vascular and fibroblast functions, promoting apoptosis (apoptosis) in cancer cells and fibroblasts. AXL/Angiokinase-IN-1 features low toxicity and good metabolic stability.
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BLU-654
0 ImagesCat. No.: HY-182043CAS No.: 2999638-62-7BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KITV654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KITV654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors.
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Toceranib-d8
0 ImagesToceranib-d8 is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
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CDK2/FLT4/PDGFRA-IN-1
0 ImagesCat. No.: HY-173124CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3) and PDGFRA, with IC50s of 1.672, 0.554, and 0.629 μM, respectively. CDK2/FLT4/PDGFRA-IN-1 exhibits potent antiproliferative effects against cancer cells (lung EBC-1, pancreatic ductal adenocarcinoma AsPC-1, colorectal HT-29 cells). CDK2/FLT4/PDGFRA-IN-1 can also induce apoptosis in cancer cells.
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GW694590A
0 ImagesCat. No.: HY-160689CAS No.: 948313-24-4Synonyms: UNC10112731GW694590A (UNC10112731) is a MYC protein stabilizer that increases endogenous MYC protein levels. GW694590A also targets receptor tyrosine kinases, inhibiting DDR2, KIT and PDGFRα by 81% at 1 μM. , 68% and 67%. GW694590A is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential effects on the Fluc reporter gene.
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1-Phenyl-1H-benzimidazole-6-carboxylic acid
0 ImagesCat. No.: HY-187149CAS No.: 220495-76-11-Phenyl-1H-benzimidazole-6-carboxylic acid is a PDGF inhibitor.
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Sennoside B (Standard)
0 ImagesSennoside B (Standard) is the analytical standard of Sennoside B. This product is intended for research and analytical applications. Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
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PDGFR Y1021 peptide (phosphorylation)
0 ImagesCat. No.: HY-P10270CAS No.: 147428-10-2PDGFR Y1021 peptide (phosphorylation) is the phosphorylated fragment of platelet-derived growth factor receptor (PDGFR). PDGFR Y1021 peptide (phosphorylation) supports association of PLCγ to PDGFR through PLCγSH2 domains, and thus promotes the production of inositol phosphates and mitogenic response.
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PDGFRα/FLT3-ITD-IN-1
0 ImagesCat. No.: HY-145902CAS No.: 2761259-05-4PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
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PDGFRalpha V561D Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70764PDGFRalpha is a receptor tyrosine kinases that stimulate cell survival, proliferation and motility. Upon PDGF binding, the receptor dimerizes and undergoes a conformational change, which activates the kinase domain. PDGFRalpha V561D is a mutant of PDGFRalpha. PDGFRalpha V561D Recombinant Human Active Protein Kinase is a recombinant PDGFRalpha V561D protein that can be used to study PDGFRalpha V561D-related functions.
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Xanthinol Nicotinate (Standard)
0 ImagesXanthinol Nicotinate (Standard) is the analytical standard of Xanthinol Nicotinate. This product is intended for research and analytical applications. Xanthinol Nicotinate (Xanthinol Niacinate), a vasodilator, can act directly on the smooth muscle of small arteries and capillaries. Xanthinol Nicotinate expands blood vessels, improves blood rheology and reduces peripheral vascular resistance.
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Pdgfra Mouse Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS10255Pdgfra Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pdgfra gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
