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PDGFR

Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor (PDGF) family. PDGF subunits -A and -B are important factors regulating cell proliferation, cellular differentiation, cell growth, development and many diseases including cancer. There are two forms of the PDGF-R, alpha and beta each encoded by a different gene. Depending on which growth factor is bound, PDGF-R homo- or heterodimerizes.

  • Regorafenib
    T1792755037-03-7
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
    • $30
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  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic iron death.
    • $34
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  • Avapritinib
    T51091703793-34-3
    Avapritinib (BLU-285) is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
    • $80
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  • Lenvatinib
    T0520417716-92-8
    Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.
    • $40
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  • Sennoside B
    T2734128-57-4
    Sennoside B is an anthranoid. Anthranoid derivatives are used all over the world as a treatment for constipation.
    • $60
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  • Pazopanib
    T0097L444731-52-6
    Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
    • $42
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  • Nintedanib
    T1777656247-17-5
    Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
    • $38
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  • CP-547632
    T10870L252003-65-9In house
    CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.
    • $30
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  • Imatinib impurities3
    T67847404844-11-7
    Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.
    • $50
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  • KN1022
    T60110205255-11-4
    KN1022 is an inhibitor of phosphorylation of platelet-derived growth factor (PDGF) receptor with IC50 of 0.26 μM.
    • $117
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  • N-Desethylsunitinib hydrochloride
    T12145L1261432-05-6
    N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.
    • $133
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  • TG 100572 Hydrochloride
    T13156L867331-64-4In house
    TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).
    • $399
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  • ZM323881 hydrochloride
    T1991193000-39-4In house
    ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.
    • $66
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  • AXL-IN-13
    T733002376928-82-2In house
    AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.
    • $79
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  • Imatinib Mesylate
    T1621220127-57-1
    Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).
    • $54
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  • Axitinib
    T1452319460-85-0
    Axitinib (AG-013736) is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.
    • $33
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  • Imatinib
    T6230152459-95-5
    Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.
    • $36
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  • Crenolanib
    T2677670220-88-9
    Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα/β and FLT3 (IC50s: 11, 3.2, and 4 nM).
    • $53
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  • TAK-632
    T18861228591-30-7
    TAK-632 is a potent pan-Raf inhibitor.
    • $35
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  • Sunitinib
    T0374L557795-19-4
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
    • $53
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  • AG-1478
    T2047153436-53-4
    AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
    • $45
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  • Ponatinib
    T2372943319-70-8
    Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
    • $50
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  • NVP-ACC789
    T3463300842-64-2
    ACC-789 (NVP-ACC789 (ZK202650); ZK-202650) is an effective, specific and orally active inhibitor of the VEGF receptor tyrosine kinases.
    • $39
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  • Ki20227
    T4315623142-96-1
    Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.
    • $39
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  • KG5
    T41003877874-85-6
    KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
    • $48
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  • SU14813
    T7945627908-92-3
    SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT).
    • $47
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  • Multi-kinase inhibitor 1
    T4191778274-97-8
    Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.
    • $33
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  • Olaratumab
    T767611024603-93-7
    Olaratumab(IMC-3G3) is a human monoclonal IgG1 antibody against platelet-derived growth factor receptor alpha (PDGFRα), which has antitumor effects and can be used to study advanced soft tissue sarcomas.
    • $372
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  • CT52923
    T60226205256-55-9
    CT52923 is a selective, orally active antagonist of platelet-derived growth factor receptor (PDGFR), functioning as an ATP-competitive inhibitor. It has versatile applications for researching an array of pathological diseases such as atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer.
    • $30
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  • Sunitinib Malate
    T0374341031-54-7
    Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
    • $37
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  • Masitinib mesylate
    T85441048007-93-7
    Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
    • $30
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  • GNF-5837
    T60971033769-28-6
    GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
    • $43
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    TargetMol | Citations Cited
  • Bisindolylmaleimide I
    T6513133052-90-1
    Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
    • $61
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    TargetMol | Citations Cited
  • AC710
    TQ02351351522-04-7
    AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
    • $30
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  • SU14813 maleate
    TQ0080849643-15-8
    SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
    • $53
    5 days
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  • PD-161570
    T23127192705-80-9
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.
    • $98
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  • Seralutinib
    T89001619931-27-9
    Seralutinib (GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.
    • $42
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  • Regorafenib monohydrate
    T1792L1019206-88-2
    Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
    • $30
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  • Sorafenib tosylate
    T0093475207-59-1
    Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
    • $37
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  • Trapidil
    T008015421-84-8
    Trapidil (Avantrin) is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.
    • $42
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  • PP58
    T13824212391-58-7
    PP58 is an inhibitor of PDGFR, FGFR and Src family.
    • $39
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  • Tyrphostin AG1433
    T13238168835-90-3
    Tyrphostin AG1433 (AG1433) is an inhibitor of tyrosine kinases and also a dual inhibitor of PDGFRβ(IC50s = 5.0 μM) and VEGFR-2 (Flk-1/KDR)(IC50s = 9.3 μM).
    • $44
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  • Ilorasertib
    TQ00591227939-82-3
    Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A/Aurora B/Aurora C (IC50s: 120 nM/7 nM/1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).
    • $55
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  • 5Z-7-Oxozeaenol
    T14055253863-19-3
    5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.
    • $215
    35 days
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  • Tivozanib
    T2456475108-18-0
    Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
    • $34
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  • Linifanib
    T2514796967-16-3
    Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).
    • $43
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  • PP121
    T24151092788-83-4
    PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
    • $51
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    TargetMol | Citations Cited
  • PDGFRα kinase inhibitor 1
    T123962209053-93-8
    PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ with IC50s of 132 nM and 6115 nM , respectively).
    • $198
    5 days
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  • CHIR-124
    T6350405168-58-3
    CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
    • $35
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  • XL019
    T3072945755-56-6
    XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
    • $68
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