VEGFR Inhibitor

VEGFR/PDGFR-IN-1 (Compound 1) is the inhibitor for VEGFR with an IC₅₀ of 0.4 μM. VEGFR/PDGFR-IN-1 inhibits angiogenesis in HUVEC cell, exhibiting potential in tumor growth and metastasis inhibition.

ZM323881 is a potent and selective VEGFR2 inhibitor with an IC₅₀ of less than 2 nM.

Golvatinib (Standard) is the analytical standard of Golvatinib. This product is intended for research and analytical applications. Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.

PX-478 (Standard) is the analytical standard of PX-478 (HY-10231). This product is intended for research and analytical applications. PX-478 is a multifunctional HIF-1α inhibitor with properties including radiosensitization, autophagy activation, and lipid accumulation inhibition. PX-478 also blocks hypoxia-induced VEGF production and regulates β-cell phenotypes under hypoxic conditions. PX-478 induces cell cycle arrest and DNA damage, restores autophagic function, reduces foam cell formation, and maintains glucose homeostasis. PX-478 is widely used in research on related diseases such as human tumors (e.g., prostate cancer), type 2 diabetes, and atherosclerosis.

Pazopanib-d₃ (GW786034-d₃) is deuterium labeled Pazopanib. 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.

Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.

XL 999 (Standard) is the analytical standard of XL 999 (HY-100315). This product is intended for research and analytical applications. XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.

Vatalanib (Standard) is the analytical standard of Vatalanib (HY-10203). This product is intended for research and analytical applications. Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC₅₀ of 37 nM.

cis-SU4312 ((Z)-SU4312) inhibits PDGFR and FLK-1 with IC₅₀s of 19.4 and 0.8 μM, respectively. cis-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC₅₀s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively. cis-SU4312 can cross blood brain barrier.

ZM 306416 (Standard) is the analytical standard of ZM 306416. This product is intended for research and analytical applications. ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.

TG 100801 Hydrochloride is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has 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.

PF 477736 (PF 00477736) (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a K_i of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), 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 exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

Lucitanib (Standard) is the analytical standard of Lucitanib. This product is intended for research and analytical applications. Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

VT3989 (Standard) is the analytical standard of VT3989 (HY-400902). This product is intended for research and analytical applications. VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors.

BRN-103 is a nicotinamide derivative and an inhibitor of the VEGF/VEGFR2 angiogenesis signaling pathway. BRN-103 concentration-dependently inhibits VEGF-induced migration, proliferation and capillary-like tube formation of HUVECs, and suppresses microvascular sprouting of ex vivo aortic rings. BRN-103 inhibits VEGF-induced phosphorylation of VEGFR2 Tyr1175, as well as the downstream phosphorylation of AKT Ser473 and eNOS Ser1172, while exerting a weak inhibitory effect on ERK phosphorylation. BRN-103 can be used in studies related to VEGF/VEGFR2 signaling and angiogenesis.

CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC₅₀ value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma.

Vandetanib (Standard) is the analytical standard of Vandetanib. This product is intended for research and analytical applications. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM).

ZM323881 (hydrochloride) (Standard) is the analytical standard of ZM323881 (hydrochloride). This product is intended for research and analytical applications. ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.