VEGFR Inhibitor

Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects.

Fursultiamine is a vitamin B₁ derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B₁?deficiency, osteoarthritis (OA) and cancer research.

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study.

SYHA1813 is a dual inhibitor of CSF1R and VEGFR. SYHA1813 has potent antitumor activity against GBM.

Bucillamine (SA96) is an orally active and potent sulfhydryl donor and antioxidant. Bucillamine is also an antirheumatic agent with antiangiogenic properties. Bucillamine can protect against Ischemia/reperfusion (I/R) injury in high-risk organ transplants. Bucillamine inhibits the production of VEGF. Bucillamine can be used for the research of choroidal neovascularization (CNV) and rheumatoid arthritis (RA).

RC148 is a humanized IgG1 bispecific antibody targeting VEGF and PD-1. RC148 blocks PD-1-PD-L1 and VEGF-VEGFR interactions, triggers VEGF-dependent enhanced PD-1 binding, enables VEGF crosslinking, and inhibits PD-1-mediated immunosuppression. RC148 can be used for the research of metastatic gastric/gastroesophageal junction adenocarcinoma, non-small cell lung cancer, and metastatic breast cancer.

Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats.

Palverafusp alfa (IMM-2510; SYN-2510) is a PD-L1/VEGF-targeting IgG1κ type humanized antibody. Palverafusp alfa blocks PD-1/PD-L1 binding, relieves immune suppression, mediates PD-L1-directed antibody-dependent cellular cytotoxicity (ADCC). Palverafusp alfa blocks VEGF/VEGFR binding, inhibits angiogenic signaling, relieves VEGF-induced immune suppression. Palverafusp alfa reduces endothelial cell proliferation, enhances ADCC and antibody-dependent cellular phagocytosis (ADCP), inhibits tumor growth, reverses T cell immune suppression. Palverafusp alfa exhibits immune stimulatory, antiangiogenic, and anti-tumor activity in the tumor microenvironment. Palverafusp alfa can be used for the research of cancer, such as solid tumors, non-small cell lung cancer.

(S)-SAR131675 is the S-enantiomer of SAR131675 (HY-15458), a potent and selective VEGFR3 inhibitor and a click chemistry reagent.

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.

Low molecular weight protamine (LMWP;TDSP5) is a truncated arginine-rich protamine peptide, as well as a heparin/low-molecular-weight heparin antidote and a cell-penetrating delivery carrier. Low molecular weight protamine neutralizes heparin-induced anticoagulant activities, including aPTT, anti-Xa and anti-IIa activities, and also neutralizes anti-Xa activity of commercially available low-molecular-weight heparin preparations. Low molecular weight protamine translocates across mammalian cell membranes, delivers conjugated impermeable molecules across tumor tissues, enhances skin permeability of conjugated epidermal growth factor, and accelerates wound healing when conjugated with epidermal growth factor. Low molecular weight protamine retains the in vitro cell proliferation activity of conjugated EGF, and also enables site-specific conjugation with peptides or proteins via genetic recombination. Low molecular weight protamine can be used in studies related to colon adenocarcinoma, skin wounds and diabetic skin wounds.

Ziv-aflibercept is a soluble inhibitor of vascular endothelial growth factor (VEGF). Ziv-aflibercept is an adaptive variant of Aflibercept (HY-108801), Ziv-aflibercept has a low PH value and high osmotic pressure when compared to Aflibercept. Ziv-aflibercept has potential applications in metastatic colorectal carcinoma and retinal diseases.

Nintedanib-d₈ is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.

Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

Tarcocimab (OG1953) is a humanized anti-VEGFA monoclonal antibody (IgG1 type). Tarcocimab is available for research in retinal vein occlusion (RVO) and wet age-related macular degeneration (AMD).

cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers.

MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC₅₀ value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer.