| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H32N2O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
IDF-11774 is a novel inhibitor of hypoxia-inducible factor α (HIFα)-1, with an IC50 of 3.65 μM. It is supplied as a white to off-white solid (C23H32N2O2, MW 368.51) at 99.30% purity.
Physical & Chemical Properties
| CAS Number | 1429054-28-3 |
|---|---|
| Molecular Formula | C23H32N2O2 |
| Molecular Weight | 368.51 g/mol |
| Purity | 99.30% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CN1CCN(C(COC2=CC=C(C3(C4)CC5CC4CC(C5)C3)C=C2)=O)CC1 |
| Target | HIF-1α |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 60 mg/mL (162.82 mM; Requires sonication and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 60 mg/mL (162.82 mM) | requires sonication and warming; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1.67 mg/mL (4.53 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (16.7 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1.67 mg/mL (4.53 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (16.7 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 1.67 mg/mL (4.53 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.67 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (16.7 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
IDF-11774 is a novel inhibitor of hypoxia-inducible factor (HIF)-1 with an IC50 of 3.65 μM in a cancer cell line. IDF-11774 has received approval as a clinical candidate for a phase I study. Capillary network formation on Matrigel is lower in human umbilical vascular endothelial cells (HUVECs) treated with IDF-11774. IDF-11774 treatment lowers mRNA expression of GLUT1 and pyruvate dehydrogenase kinase 1 (PDK1). Intracellular ATP levels are also significantly lower when IDF-11774 is present, and the reduction is greater under low glucose conditions (5.5 mM)[1].
In Vivo
In tumors of mice given oral IDF-11774, luciferase activity and HIF-1α accumulation are strongly suppressed compared with the control. Daily oral administration of IDF-11774 for two weeks produces significant dose-dependent tumor regression in the mouse model[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[1]
Use female Balb/c nude mice. Generate tumors by subcutaneous injection of cancer cells into 4- to 6-week-old female Balb/c nude mice (5 mice per group). When the tumors reach 100 mm3, administer IDF-11774 orally (per oral) or intravenously for 15 days. Determine tumor volumes (V) with the equation V (mm3)=(length×width×height)×0.5. Calculate percentage tumor growth inhibition (%TGI) values for each treatment group versus the control[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Phosphodiesterase 10A Is a Key Mediator of Lung Inflammation. J Immunol 2021 Jun 15;206(12):3010-3020. PMID: 34117108
Research Square Preprint. 2023 Jun 20.