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 (64)
Related Products (64)
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Recombinant Proteins (12)
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Lenvatinib
0 ImagesSynonyms: E7080; MK-7902
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Nintedanib
0 ImagesSynonyms: BIBF 1120Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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Nintedanib esylate
0 ImagesSynonyms: BIBF 1120 esylateNintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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Lenvatinib mesylate
0 ImagesSynonyms: E7080 mesylate; MK-7902 mesylate
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Multi-kinase-IN-15
0 ImagesCat. No.: HY-131571CAS No.: 1613168-52-7Multi-kinase-IN-15 is an orally active multi-kinase inhibitor. Multi-kinase-IN-15 inhibits the kinase activity of MNK1, MNK2, ABL1, ABL1 T315I, FLT3, VEGFR2, RET, cKIT, FGFR2, PDGFRα, and PDGFRβ. Multi-kinase-IN-15 dose-dependently reduces phosphorylation of eIF4E and phosphorylated Crkl in tumor cells, and decreases phosphorylation of eIF4E in tumor tissues. Multi-kinase-IN-15 inhibits tumor growth. Multi-kinase-IN-15 can be used for research on chronic myeloid leukemia.
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Crenolanib
0 ImagesSynonyms: CP-868596
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Ripretinib
0 ImagesSynonyms: DCC-2618Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
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Velzatinib
0 ImagesSynonyms: M4205; IDRX-42
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Ponatinib hydrochloride
0 ImagesSynonyms: AP24534 hydrochloride
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Tyrphostin AG1296
0 ImagesSynonyms: AG1296Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
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Seralutinib
0 ImagesSynonyms: GB002; PK10571Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
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Amuvatinib
0 ImagesSynonyms: MP470; HPK 56Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
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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.
