Description
IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
Product information
CAS Number: 1429054-28-3
Molecular Weight: 368.51
Formula: C23H32N2O2
Chemical Name: 2-[4-(adamantan-1-yl)phenoxy]-1-(4-methylpiperazin-1-yl)ethan-1-one
Smiles: CN1CCN(CC1)C(=O)COC1C=CC(=CC=1)C12CC3CC(C1)CC(C2)C3
InChiKey: QGBBBLPWBSWERZ-UHFFFAOYSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 60 mg/mL (162.82 mM; Need ultrasonic and warming).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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