ENMD-2076
| CAS号 | 934353-76-1 | 货号 | BCP06358 |
| 中文名 | ENMD-2076 | ||
| 英文名 | ENMD-2076 | ||
| 中文别名 | |||
| 英文别名 | ENMD 2076;ENMD2076; | ||
| 分子式 | C21H25N7 | 分子量 | 375.47 |
| 生物活性 | ENMD-2076 indicates activity against multiple kinases involved in angiogenesis, including FLT3, RET, FLT4/VEGFR3, SRC, NTRK1, CSF1R/FMS, LCK, VEGFR2/KDR, FGFR1/2, and PDGFRα with IC50 from 1.86-120 nM. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. ENMD-2076 induces regression or complete inhibition of tumor growth in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines.ENMD-2076 is the L (+) tartrate salt of ENMD-981693. ENMD-2076 shows significant cytotoxicity against myeloma cell lines (IM9, ARH-77, U266, RPMI 8226, MM.1S, MM.1R, NCI-H929) and primary cells with IC50 from 2.99 to 7.06 μM, which induces apoptosis. ENMD-2076 indicates low cytotoxicity to haematopoietic progenitors. ENMD-2076 inhibits the phosphoinositide 3-kinase/Akt pathway and downregulates survivin and X-linked inhibitor of apoptosis | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | Src/Bcr Abl Aurora PDGFR VEGFR FLT3 FGFR | ||
结构式
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