| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H22O7 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) that blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. It upregulates cleaved-PARP and p-P38, induces apoptosis, and has anticancer activity against non-small cell lung cancer[1]. It is supplied as a white to off-white solid (C20H22O7, MW 374.38) at 99.16% purity.
Physical & Chemical Properties
| CAS Number | 3078120-01-8 |
|---|---|
| Molecular Formula | C20H22O7 |
| Molecular Weight | 374.38 g/mol |
| Purity | 99.16% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C1C[C@H](C2=CC=C(OC)C=C2)OC3=C1C(OCOC)=CC(OCOC)=C3 |
| Signaling Pathway | Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor; Apoptosis; PI3K/Akt/mTOR; Epigenetics; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 100 mg/mL (267.11 mM; Requires sonication; 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, 6 months; -20°C, 1 month. |
| 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 | 100 mg/mL (267.11 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); 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 | 2.5 mg/mL (6.68 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (25.0 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 | 2.5 mg/mL (6.68 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (25.0 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 | 2.5 mg/mL (6.68 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
ARI-1 (0.1-100 μM；72 h) blocks the PI3K/AKT/mTOR pathway, which inhibits proliferation and induces apoptosis in H1975 and PC9 cells[1].
Apoptosis Analysis[1]
| Cell Line | H1975, PC9 |
|---|---|
| Concentration | 15 μM |
| Incubation Time | 72 h |
| Result | Induced apoptosis in H1975 and PC9 cells, with apoptosis rates increasing from 4.89% to 33.27% and from 0.49% to 12.43%, respectively. |
Western Blot Analysis[1]
| Cell Line | H1975, PC9 |
|---|---|
| Concentration | 15 μM |
| Incubation Time | 72 h |
| Result | Downregulated the levels of p-AKT, p-mTOR, and PCNA, and upregulated cleaved-PARP and p-P38. |
In Vivo
In BALB/c nude mice inoculated subcutaneously with H1975 cells, ARI-1 (i.v., 5 mg/kg every 2 days for 14 days) significantly inhibits tumor growth, with no obvious organ toxicity[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Anti-NSCLC efficacy of a novel ROR1/PI3Kα/BRD4 multi-target inhibitor. Bioorg Med Chem 2026 Jan 1:132:118483. PMID: 41240398
