CAS NO: | 1429054-28-3 |
规格: | ≥98% |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Name: IDF-11774 CAS#: 1429054-28-3 Chemical Formula: C23H32N2O2 Exact Mass: 368.2464 Molecular Weight: 368.521 | |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Technical Information | Synonym: IDF11774; IDF 11774; IDF-11774 Chemical Name: 2-(4-((3r,5r,7r)-adamantan-1-yl)phenoxy)-1-(4-methylpiperazin-1-yl)ethan-1-one InChi Key: QGBBBLPWBSWERZ-KIOFGVERSA-N InChi Code: InChI=1S/C23H32N2O2/c1-24-6-8-25(9-7-24)22(26)16-27-21-4-2-20(3-5-21)23-13-17-10-18(14-23)12-19(11-17)15-23/h2-5,17-19H,6-16H2,1H3/t17-,18-,19-,23? SMILES Code: O=C(N1CCN(C)CC1)COC2=CC=C(C34C[C@H]5C[C@@](C4)([H])C[C@H](C5)C3)C=C2 |
Target | IC50: 3.65 μM (HIF-1α) |
---|---|
In Vitro | IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC50 of 3.65 μM in cancer cell line. IDF-11774 has been approved as a clinical candidate for a phase I study. Human umbilical vascular endothelial cells (HUVECs) treated with IDF-11774 show reduced capillary network formation on Matrigel. IDF-11774 treatment leads to reduced mRNA expression of GLUT1 and pyruvate dehydrogenase kinase 1 (PDK1). In addition, intracellular ATP levels are significantly reduced in the presence of IDF-11774 and are affected to a greater degree under low glucose conditions (5.5 mM). |
In Vivo | Luciferase activity and HIF-1α accumulation are strongly suppressed
in the tumors of mice treated by oral administration of IDF-11774,
compare with the control. When IDF-11774 is orally administered daily
for two weeks, significant dose-dependent tumor regression is observed
in the mouse model. |