Molecular Formula | C21H25N7 |
Molar Mass | 375.47 |
Density | 1.267 |
Storage Condition | -20℃ |
In vitro study | ENMD-2076 a number of kinases effective in angiogenesis, including VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2, and PDGFRα, have an IC50 of 1.86 to 120 nM. ENMD-2076 inhibits a variety of human solid tumor and blood cancer cell lines with IC50 of 0.025 to 0.7 μm, induces apoptosis, and stops the cell cycle at G2/M phase. ENMD-2076 effect on breast cancer, colon cancer, melanoma, leukemia, multiple myeloma cell line transplantation tumor model, induce tumor regression or completely inhibit tumor growth. ENMD-2076 is the L ( ) tartrate salt form of ENMD-981693. ENMD-2076 showed significant cytotoxicity in myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells with IC50 of 2.99 to 7.06 μm, apoptosis was induced. ENMD-2076 effect on hematopoietic precursor cells showed low cytotoxicity. ENMD-2076 inhibit PI3K/AKT pathway and down-regulate apoptosis inhibitory protein. ENMD-2076 also inhibited aurora A and B kinases and induced cell cycle arrest at G2/M phase. ENMD-2076 a number of kinases active in angiogenesis, including VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2, and PDGFRα, have an IC50 of 1.86 to 120 nM. ENMD-2076 inhibits a variety of human solid tumor and blood cancer cell lines with IC50 of 0.025 to 0.7 μm, induces apoptosis, and stops the cell cycle at G2/M phase. ENMD-2076 effect on breast cancer, colon cancer, melanoma, leukemia, multiple myeloma cell line transplantation tumor model, induce tumor regression or completely inhibit tumor growth. ENMD-2076 is the L ( ) tartrate salt form of ENMD-981693. ENMD-2076 effect on myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells, showed significant cytotoxicity with IC50 of 2.99 to 7.06 μm, inducing apoptosis. ENMD-2076 effect on hematopoietic precursor cells showed low cytotoxicity. ENMD-2076 inhibit PI3K/AKT pathway and down-regulate apoptosis inhibitory protein. ENMD-2076 also inhibited aurora A and B kinases and induced cell cycle arrest at G2/M phase. |
In vivo study | ENMD-2076 had a long-lasting inhibitory effect on the activation of Flt3,VEGFR2/KDR and FGFR1/2 in HT29 xenograft model. ENMD-2076 acting on the MDA-MB-231 transplanted tumor model can block the formation of new blood vessels, and the formation of blood vessels. H929 human plasma cell xenografts were treated orally on ENMD-2076 (50, 100,200 mg/kg daily). Inhibits tumor growth, and significantly reduces phospho-histone 3 (pH3), Ki-67, and angiogenesis, and significantly increases cleaved caspase-3. ENMD-2076 had a long-lasting inhibitory effect on Flt3,VEGFR2/KDR and FGFR1/2 activation in HT29 xenograft model. ENMD-2076 acting on the MDA-MB-231 transplanted tumor model can block the formation of new blood vessels, and the formation of blood vessels. H929 human plasma cell xenografts were treated orally on ENMD-2076 (50, 100,200 mg/kg daily). Inhibits tumor growth, and significantly reduces phospho-histone 3 (pH3), Ki-67, and angiogenesis, and significantly increases cleaved caspase-3. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.663 ml | 13.317 ml | 26.633 ml |
5 mM | 0.533 ml | 2.663 ml | 5.327 ml |
10 mM | 0.266 ml | 1.332 ml | 2.663 ml |
5 mM | 0.053 ml | 0.266 ml | 0.533 ml |