PDGFR Inhibitor

Amuvatinib 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.

Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET^V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.

Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, 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. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer.

SNX-7081 is an Hsp90 inhibitor with K_i and IC₅₀ values of 26 nM and 44 nM, respectively. SNX-7081 blocks the nuclear translocation of NF-κB, inhibits the production of pro-inflammatory cytokines, attenuates the ERK/JNK and PDGF signaling pathways, and suppresses LPS (HY-D1056)-induced nitric oxide production. SNX-7081 inhibits DNA repair, induces G₂/M cell cycle arrest, and triggers apoptosis via downregulation of MYC/nucleolin and activation of Fas. SNX-7081 can be used in research related to rheumatoid arthritis and cancer.

SU10944 is a selective, orally active VEGFR inhibitor, with an IC₅₀ of 6 nM against VEGFR-1, an IC₅₀ of 96 nM and a K_i of 21 nM against VEGFR-2. SU10944 only exhibits weak inhibitory activity against PDGFRβ (IC₅₀ = 1 μM), SCFR (IC₅₀ = 1.58 μM) and FGFR-1 (IC₅₀ = 1.6 μM). SU10944 selectively inhibits VEGFR receptor downstream signaling, neovascularization, vascular permeability, VEGF-mediated tissue factor production, and induces tumor growth delay. SU10944 can be used in research related to diabetic retinopathy, exudative age-related macular degeneration or cancer.

Linifanib (ABT-869) (GMP) is Linifanib (HY-50751) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Linifanib is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC₅₀s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (GMP) promotes the generation and reprogramming of iPSCs from somatic cells.

SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC₅₀ of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.

Henatinib maleate is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib maleate inhibits the activity of VEGFR-2, c-kit, PDGFR with IC₅₀ values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib maleate significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway.

BOT1711 is a human IgG1κ monoclonal antibody targeting PDGFRB/CD140b. PDGFRB/CD140b belongs to type I receptor tyrosine kinases (RTKs), and is mainly expressed in vascular smooth muscle cells, pericytes, fibroblasts, certain mesenchymal stem cells, and tumor stromal cells.

Multi-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.

PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC₅₀s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.

Lenvatinib-d₅ is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (K_i= 0.009 µM for VEGFR-1/2/3), PDGFR (K_i= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.

KIT/PDGFRA-IN-2 is a tyrosine kinase inhibitor targeting KIT and PDGFRA. KIT/PDGFRA-IN-2 inhibits the downstream signaling pathways of PDGFRA mutants, including the phosphorylation of AKT, MAPK and S6. KIT/PDGFRA-IN-2 can be used in the research of gastrointestinal stromal tumors.

KIT/PDGFRA-IN-1 (compound 19) is a stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA) inhibitor. KIT/PDGFRA-IN-1 inhibits KIT-wt, KIT-D816H, KIT-T670I, PDGFRA-wt, PDGFRA-D842V, PDGFRA-T674I and PDGFRA-G680R with IC₅₀s of 2.3, 12, 492, 0.8, 99.9, 42.3, and 4.3 μM, respectively. KIT/PDGFRA-IN-1 inhibits GIST-T1, T1-a-D842V and GIST-48B cells (PDGFR- and KIT-Mutant GIST cell Lines) with GR₅₀s of 12, 8900, ≥10 000 nM, respectively.

Pegpleranib (Fovista) is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.

PDGFRα 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.

PDGFRA-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.

SU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC₅₀ values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma.

L-783277 (Compound 4) is a MEK inhibitor (IC₅₀ = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC₅₀ = 22 mM) and cell proliferation (IC₅₀ = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.