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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Ponatinib-d8
0 ImagesSynonyms: AP24534-d8
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Dovitinib lactate hydrate
0 ImagesCat. No.: HY-B0062CAS No.: 915769-50-5Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate
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GZD856
0 ImagesCat. No.: HY-101489CAS No.: 1257628-64-0
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Amuvatinib hydrochloride
0 ImagesCat. No.: HY-10206ACAS No.: 1055986-67-8Synonyms: MP470 hydrochloride; HPK 56 hydrochlorideAmuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
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Multi-kinase inhibitor 3
0 ImagesCat. No.: HY-168114CAS No.: 2648279-76-7Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity.
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PDGFRα kinase-IN-2
0 ImagesCat. No.: HY-175540CAS No.: 3066103-58-7PDGFRα kinase-IN-2 is a potent PDGFR-α inhibitor with an IC50 of 2.1 nM. PDGFRα kinase-IN-2 exhibits anticancer activity against human colon cancer HT-29 cell with an IC50 of 1.48 μM. PDGFRα kinase-IN-2 has anti-angiogenic activity in zebrafish models and low embryonic lethality. PDGFRα kinase-IN-2 can used for the studies of colon cancer and anti-angiogenesis.
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PDGFRA-IN-1
0 ImagesCat. No.: HY-175212PDGFRA-IN-1 (Compound 4p) is a Platelet-derived growth factor receptor A (PDGFRA) inhibitor with an IC50 of 1.25 μM. PDGFRA-IN-1 has a significant anticancer activity and potently kills cancer cells including primary patient-derived glioma cells.
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Multi-kinase-IN-1
0 ImagesCat. No.: HY-146014CAS No.: 2470807-67-9Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer.
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Ki11502
0 ImagesKi11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
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MET/PDGFRA-IN-2
0 ImagesCat. No.: HY-149511CAS No.: 3125694-57-4
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HSN748
0 ImagesCat. No.: HY-171146CAS No.: 2409925-53-5HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia.
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GSK190937
0 ImagesCat. No.: HY-181108CAS No.: 2651234-01-2GSK190937 is a type II platelet-derived growth factor receptor alpha (PDGFRA) human kinase inhibitor with antimalarial activity. GSK190937 can inhibit the formation of hemozoin in the malaria parasite, resulting in the accumulation of free hemoglobin within the malaria parasite. GSK190937 shows IC50 values of 0.22, 0.59 and 0.25 μM against P. falciparum NF54, K1 and Dd2 parasite. GSK190937 shows an IC50 of 25 μM for CHO cells. GSK190937 can be used for research of malaria.
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KBP-7018 hydrochloride
0 ImagesCat. No.: HY-117873ACAS No.: 1613437-67-4KBP-7018 hydrochloride is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC50 value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 hydrochloride improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 hydrochloride can be used in research related to idiopathic pulmonary fibrosis.
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Multi-kinase-IN-2
0 ImagesCat. No.: HY-150026CAS No.: 2095628-21-8Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
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VEGFR2-IN-84
0 ImagesCat. No.: HY-182354CAS No.: 861877-12-5VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors.
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Antifibrotic agent 1
0 ImagesCat. No.: HY-176194Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model.
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MET/PDGFRA-IN-1
0 ImagesCat. No.: HY-149510CAS No.: 3125694-48-3MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively).
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IHMT-TRK-284
0 ImagesCat. No.: HY-146697CAS No.: 2416844-79-4
