VEGFR Inhibitor

Foretinib (Standard) is the analytical standard of Foretinib. This product is intended for research and analytical applications. Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.

Orantinib (Standard) is the analytical standard of Orantinib (HY-10517). This product is intended for research and analytical applications. Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

OSI-930 (Standard) is the analytical standard of OSI-930 (HY-10204). This product is intended for research and analytical applications. OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC₅₀s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.

GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC₅₀ of 1.03 μM and 2 nM, respectively. GSK248233A also shows activity against the AGC family. GSK248233A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays.

Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.

Acrizanib hydrochloride (LHA510 hydrochloride) is a small-molecule vascular endothelial growth factor receptor 2 (VEGFR-2, KDR) inhibitor. Acrizanib hydrochloride inhibits the proliferation of BaF3-Tel-KDR cells dependent on VEGFR-2 activity, with an IC₅₀ of 17.4 nM. Acrizanib hydrochloride can be used in research related to choroidal neovascularization and neovascular age-related macular degeneration.

Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.

SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC₅₀ values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC₅₀ values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.

(Z)-Orantinib (Standard) is the analytical standard of (Z)-Orantinib (HY-10517A). This product is intended for research and analytical applications. (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

Tivozanib (Standard) is the analytical standard of Tivozanib. This product is intended for research and analytical applications. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy.

CZC-8004 (Standard) is the analytical standard of CZC-8004 (HY-111138). This product is intended for research and analytical applications. CZC-8004 (CZC-00008004) is a pan-K_inase inhibitor. CZC-8004 has IC₅₀ values of 650 and 437 nM for EGFR WT and VEGFR2 V916M, respectively. CZC-8004 can be used in the study of cancer.

Talmapimod (Standard) is the analytical standard of Talmapimod (HY-10406). This product is intended for research and analytical applications. Talmapimod (SCIO-469) is an orally active and selective inhibitor of p38α MAPK with an IC₅₀ of 9 nM. Talmapimod inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. Talmapimod inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).

(±)-Glaziovine, a proaporphine alkaloid, has anxiolytic activity. (±)-Glaziovine can be used for neuropharmacological research.

Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) 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.

4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC₅₀ = 1.12 μM) and COX-2 (IC₅₀ = 0.83 μM)), NF-κB (IC₅₀ = 88.7 μM) and cytokine production (TNF-α (IC₅₀ = 96.84 μg/mL) and IL-1β (IC₅₀ = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats.

RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PlGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC₅₀ values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity.

Oglufanide (H-Glu-Trp-OH) disodium is a dipeptide immunomodulator isolated from calf thymus. Oglufanide disodium inhibits vascular endothelial growth factor (VEGF). Oglufanide disodium can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide disodium shows antitumor and anti-angiogenesis activities.

Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.

VEGFR-IN-7 (Compound 2) is a VEGFR inhibitor, showing inhibition of angiogenesis to a lesser extent. VEGFR-IN-7 is promising for research of cardiovascular diseases.

BMS-794833 (Standard) is the analytical standard of BMS-794833 (HY-10497). This product is intended for research and analytical applications. BMS-794833 is a VEGFR2 and Met inhibitor extracted from patent WO2009094417, compound example 1; has IC₅₀s of 15 and 1.7 nM, respectively.