PDGFR Inhibitor

Tandutinib (MLN518) sulfate is a potent and selective inhibitor of the FLT3 with an IC₅₀ of 0.22 μM, and also inhibits c-Kit and PDGFR with IC₅₀s of 0.17 μM and 0.20 μM, respectively. Tandutinib sulfate can be used for acute myelogenous leukemia (AML). Tandutinib sulfate has the ability to cross the blood-brain barrier.

Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

Telatinib (mesylate) (Standard) is the analytical standard of Telatinib (mesylate). This product is intended for research and analytical applications. Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

ENMD-2076 Tartrate (Standard) is the analytical standard of ENMD-2076 (Tartrate) (HY-10987). This product is intended for research and analytical applications. ENMD-2076 Tartrate is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.

PDGFRα K_inase inhibitor 1 (Standard) is the analytical standard of PDGFRα K_inase inhibitor 1 (HY-111507). This product is intended for research and analytical applications. PDGFRα K_inase inhibitor 1 is a highly selective type II PDGFRα K_inase inhibitor with IC₅₀s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.

Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

ON012380 is a kinase inhibitor with an IC₅₀ of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia.

SU16f (Standard) is the analytical standard of SU16f (HY-108628). This product is intended for research and analytical applications. SU16f is a potent and selective PDGFRβ inhibitor with IC₅₀s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, VEGF-R2, FGF-R1, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.

AC710 Mesylate is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.

Ki20227 (Standard) is the analytical standard of Ki20227 (HY-10408). This product is intended for research and analytical applications. Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC₅₀s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.

SU14813 (Standard) is the analytical standard of SU14813 (HY-10501). This product is intended for research and analytical applications. SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.

Tyrphostin AG 1433 is a specific and potent inhibitor of PDGFR-β and of KDR/Flk-1. Tyrphostin AG 1433 acts as an angiogenesis inhibitor.