PDGFRα
PDGFRα is a cell-surface receptor tyrosine kinase that binds PDGF-A, PDGF-B, and PDGF-C ligands to regulate mesenchymal cell proliferation, migration, survival, and developmental tissue organization[1]. Mechanistically, ligand binding promotes receptor dimerization and autophosphorylation, linking PDGFRα signaling to downstream pathways that control cell growth, chemotaxis, and differentiation[1][2]. In disease models, genomic PDGFRA activation contributes to tumor progression, and extracellular-domain mutations can promote cell survival and proliferation[3]. Compared with PDGFRβ, PDGFRα shows distinct ligand specificity and activates both shared and isoform-specific signaling outputs, making isoform selection important in experimental design[1][4]. For research applications, PDGFRA inhibitors such as avapritinib support pathway validation in PDGFRA D842V-mutant gastrointestinal stromal tumor and PDGFRA-altered high-grade glioma models[5][6].
References:
- [1]. Nazari-Robati M, et al. Enhancement of thermal stability of chondroitinase ABC I by site-directed mutagenesis: an insight from Ramachandran plot. Biochim Biophys Acta. 2013 Feb;1834(2):479-86. [Content Brief]
- [2]. Eriksson A, et al. PDGF alpha- and beta-receptors activate unique and common signal transduction pathways. EMBO J. 1992 Feb;11(2):543-50. [Content Brief]
- [3]. Ip CKM, et al. Neomorphic PDGFRA extracellular domain driver mutations are resistant to PDGFRA targeted therapies. Nat Commun. 2018 Nov 2;9(1):4583. [Content Brief]
- [4]. Donovan J, et al. Platelet-derived growth factor alpha and beta receptors have overlapping functional activities towards fibroblasts. Fibrogenesis Tissue Repair. 2013 May 10;6(1):10. [Content Brief]
- [5]. Heinrich MC, et al. Avapritinib in advanced PDGFRA D842V-mutant gastrointestinal stromal tumour (NAVIGATOR): a multicentre, open-label, phase 1 trial. Lancet Oncol. 2020 Jul;21(7):935-946. [Content Brief]
- [6]. Mayr L, et al. Effective targeting of PDGFRA-altered high-grade glioma with avapritinib. Cancer Cell. 2025 Apr 14;43(4):740-756.e8. [Content Brief]
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PDGFRα Related Products (63)
Related Products (63)
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Recombinant Proteins (12)
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JNJ-10198409
0 ImagesJNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
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MT-125
0 ImagesCat. No.: HY-174406Purity: 98.73%MT-125 is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.
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Ilorasertib
0 ImagesSynonyms: ABT-348Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
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Chiauranib
0 ImagesSynonyms: Ibcasertib; CS2164Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.
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MT-125 free base
0 ImagesMT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.
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Tovetumab
0 ImagesSynonyms: MEDI-575Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC).
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HG-7-85-01
0 ImagesHG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
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Dovitinib lactate
0 ImagesSynonyms: CHIR-258 lactate; TKI-258 lactate
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Ilorasertib hydrochloride
0 ImagesSynonyms: ABT-348 hydrochlorideIlorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
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Hypothemycin
0 ImagesCat. No.: HY-107417CAS No.: 76958-67-3
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GZD856 formic
0 ImagesCat. No.: HY-101489ACAS No.: 2804039-78-7GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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BI-4659
0 ImagesBI-4659 is a TGFβRI and PDGFRα inhibitor with IC50 values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury.
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WQ-C-401
0 ImagesWQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension.
