pdgfrβ

PDGFR-IN-1 (compound 7m) is an orally active PDGFR (platelet-derived growth factor receptor) inhibitor that targets PDGFRα (IC50: 2.4 nM) and PDGFRβ (IC50: 0.9 nM), exhibiting strong anti-tumor effects and low toxicity, making it suitable for osteosarcoma studies.

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC and can be used for research on amyotrophic lateral sclerosis [1].

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets 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. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ) with IC50 values of 132 nM and 6115 nM, respectively.

PDGFRα FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα (IC50: 0.153 μM) and FLT3 (IC50: 0.004 μM), with potential applications in the study of acute myeloid leukaemia or chronic eosinophilic leukaemia.

PDGFRα/FLT3-ITD-IN-2 is a potent inhibitor of PDGFRα (IC50>20 μM) and FLT3 (IC50: 0.004 μM). PDGFRα/FLT3-ITD-IN-2 has shown investigational potential in acute myeloid leukemia or chronic eosinophilic leukemia.

PDGFRα/FLT3-ITD-IN-1 are potent inhibitors of PDGFRα/FLT3, and their IC50 values are greater than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 exhibits investigational potential in acute myeloid leukemia or chronic eosinophilic leukemia.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

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.

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.

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.

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

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.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

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.

Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1 2 3, FGFR1 2 3, and PDGFRα β.

N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.

(Z)-Semaxinib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. (Z)-Semaxinib is a quinolone derivative with potential antineoplastic activity.

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

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.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

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).

MET Tyrosine Kinase Inhibitor PF-04217903 is an orally bioavailabe, small-molecule tyrosine kinase inhibitor with potential antineoplastic activity.

Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.

Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα β and FLT3 (IC50s: 11, 3.2, and 4 nM).

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRβ, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

CP-673451 is a specific inhibitor of PDGFRα β (IC50: 10 1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.

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.

ACC-789 (NVP-ACC789 (ZK202650); ZK-202650) is an effective, specific and orally active inhibitor of the VEGF receptor tyrosine kinases.

Seralutinib (GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.

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.

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.

Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1 KDR, PDGFR

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

Vatalanib dihydrochloride (PTK787 dihydrochloride)(IC50=37 nM) is an inhibitor of VEGFR2 KDR. It exhibits less effective against VEGFR1 Flt-1 and 18-fold against VEGFR3 Flt-4.

TAK-593 is an effective VEGFR and PDGFR family inhibitor (IC50s: 3.2, 0.95, 1.1, 4.3, and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα, and PDFGRβ, respectively).

JNJ- 10198409 is a relatively selective and ATP competitive PDGF-RTK inhibitor (IC50=2 nM). JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent.

Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.

AZD2932 is a potent, multi-targeted kinase inhibitor of VEGFR2, PDGFβ, Flt-3, and c-Kit.

MAZ51 is a VEGFR-3 (Flt-4) tyrosine kinase inhibitor.

Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.