Tie Inhibitor

6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, with an IC₅₀ value of 2.1 μM. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether interacts with the ATP binding site of Tie2 kinase, inhibiting kinase activity and subsequently blocking tumor angiogenesis. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether can be isolated from sponges of the genus Dysidea.

TIE-2/VEGFR-2 kinase-IN-5 is an anti-angiogenic agent. TIE-2/VEGFR-2 kinase-IN-5 also is a potent TIE-2 and VEGFR-2 tyrosine kinase inhibitor with pIC₅₀ values of 7.78 nM and 8.11 nM, respectively. TIE-2/VEGFR-2 kinase-IN-5 can be used for the research of angiogenesis.

TP-S1-68 (Compound 10) is a TIE-2 inhibitor with an IC₅₀ of 3.65 μM. TP-S1-68 exhibits antibacterial activity against a variety of fungal and bacteria. TP-S1-68 serves as a starting compound for the further development of TIE-2 inhibitors. TP-S1-68 can be used in research related to solid tumors, bacterial infections and fungal infections.

Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.

Zerumin A is an anti-angiogenic agent that acts on multiple molecular targets related to angiogenesis (including kdr/VEGFR2, angpt1, angpt2, tie1, and tie2). Zerumin A specifically inhibits the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by regulating the VEGF-VEGFR and ANGPT-TIE signaling pathways, and dose-dependently inhibits angiogenesis (10-20 μM significantly inhibits zebrafish embryo angiogenesis). Zerumin A can be used in the research of cancer and angiogenesis-related inflammatory diseases. Zerumin A can be naturally extracted from the 95% ethanol extract of the fruits, seeds, and pericarp of Alpinia caerulea (R.Br.) Bentham (a plant of the Alpinia genus in the Zingiberaceae family).

AMG-780 is a fully human IgG2 antibody that targets angiopoietin 1 (Ang1) (IC₅₀ = 4.5 nM) and angiopoietin 2 (Ang2) (IC₅₀ = 0.06 nM). AMG-780 inhibits tumor growth in the Colo205 xenograft mouse model by inhibiting both Ang1 and Ang2. AMG-780 is indicated for the research of cancers such as colon cancer.

Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC₅₀=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis.

LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.

UBX2050 is a human monoclonal antibody (mAb) targeting TIE2. UBX2050 can be used in Age-related macular degeneration, Diabetic macular oedema and Diabetic retinopathy research.

TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC₅₀ values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis.

TIE-2/VEGFR-2 kinase-IN-4, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC₅₀ values of 5.2 nM and 5.1 nM, respectively. TIE-2/VEGFR-2 kinase-IN-4 can be used for the research of angiogenesis.

DX-2240 is a human monoclonal antibody (mAb) targeting TIE1. DX-2240 inhibits tumor growth and sensitizes tumor vasculature to anti-angiogenic agents (VEGF pathway inhibitors).

BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a K_d of 16 pM for hANG2, an EC₅₀ of 1.4 nM for VEGF₁₆₅, and an EC₅₀ of 2.3 nM for VEGF₁₂₁. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer.

Pexmetinib (Standard) (ARRY-614 (Standard)) is the analytical standard of Pexmetinib (HY-16782). This product is intended for research and analytical applications. Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

Tie2 kinase inhibitor 1 (Standard) is the analytical standard of Tie2 kinase inhibitor 1 (HY-100556). This product is intended for research and analytical applications. Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer 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.

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.

Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an ₅₀ of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects.

Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib hydrochloride inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

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.