PDGFR Inhibitor

Sennoside B (Standard) is the analytical standard of Sennoside B. This product is intended for research and analytical applications. Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.

VEGFR2-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.

PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC₅₀s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.

Xanthinol Nicotinate (Standard) is the analytical standard of Xanthinol Nicotinate. This product is intended for research and analytical applications. Xanthinol Nicotinate (Xanthinol Niacinate), a vasodilator, can act directly on the smooth muscle of small arteries and capillaries. Xanthinol Nicotinate expands blood vessels, improves blood rheology and reduces peripheral vascular resistance.

VEGFR-2-IN-89 is a VEGFR-2 inhibitor with an IC₅₀ of 77 nM. VEGFR-2-IN-89 potently inhibits c-Met kinase activity with an IC₅₀ of 0.152 μM, and also exhibits good inhibitory activity against EGFR (IC₅₀ = 0.269 μM) and PDGFR-β kinase (IC₅₀ = 0.301 μM). VEGFR-2-IN-89 displays anticancer activity against liver cancer. VEGFR-2-IN-89 can be used in the research of hepatocellular carcinoma.

Antifibrotic 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.

Pdgfra Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pdgfra gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

MET/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).

KIT/PDGFRA-IN-3 is a KIT and PDGFRA mutant kinase inhibitor, with an IC₅₀ of 9 nM against human PDGFRA. KIT/PDGFRA-IN-3 inhibits the kinase activity of KIT, exhibiting superior selectivity for mutant KIT over wild-type KIT. KIT/PDGFRA-IN-3 suppresses the kinase activity of PDGFRA and blocks downstream signaling pathways. KIT/PDGFRA-IN-3 can be used in studies of gastrointestinal stromal tumors.

PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC₅₀s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC₅₀ values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.

Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib 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 significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs).

KN1022 an inhibitor of phosphorylation of platelet-derived growth factor receptor (PDGFR) with IC₅₀ of 0.24 μM.

Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

Regorafenib-¹³C,d₃ is the ¹³C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.

2-Methyl-3-phenylquinoxaline (compound 38) is a potent platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) inhibitor with modest inhibitory activity against PDGFR kinase in intact cells (IC₅₀ greater than 100 μM).

Cediranib (maleate) (Standard) is the analytical standard of Cediranib (maleate). This product is intended for research and analytical applications. Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. Masitinib mesylate (AB-1010 mesylate) 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 mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.

Toceranib phosphate (Standard) is the analytical standard of Toceranib phosphate (HY-10330A). This product is intended for research and analytical applications. Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .

RPR-101511 is a 3-substituted quinoline derivative. RPR-101511 is a PDGF receptor tyrosine kinase inhibitor (IC₅₀: 0.001-0.02 μM).