| Field | Specification |
|---|---|
| Target | |
| Alternative names | ARQ 751 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C35H38N8O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Vevorisertib, also known as ARQ 751, is an orally active, potent, and selective pan-AKT serine/threonine kinase inhibitor active against AKT1 (IC50 0.55 nM), AKT2 (IC50 0.81 nM), and AKT3 (IC50 1.31 nM). Used alone or in combination with other anti-cancer agents, it can be used to the research of solid tumors bearing PIK3CA/AKT/PTEN mutations[1][2][3][4]. It is supplied as a light yellow to yellow solid (C35H38N8O, MW 586.73) at 98.03% purity.
Physical & Chemical Properties
| CAS Number | 1416775-46-6 |
|---|---|
| Molecular Formula | C35H38N8O |
| Molecular Weight | 586.73 g/mol |
| Purity | 98.03% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | NC1=C(C=CC=N1)C2=NC3=CC=C(C4=CC(N(CC5)CCC5N(C)C(C)=O)=CC=C4)N=C3N2C6=CC=C(C7(CCC7)N)C=C6 |
| Target | Akt1, Akt2, Akt3 |
| Signaling Pathway | PI3K/Akt/mTOR; Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 6.67 mg/mL (11.37 mM; Requires sonication and warming and heat to 60°C; 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. |
Biological Activity
IC50 & Target[4]
|
Akt1 0.55 nM (IC50) |
Akt2 0.81 nM (IC50) |
Akt3 1.31 nM (IC50) |
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.
[1]. Vevorisertib (ARQ 751) (4440-001) as a Single Agent or in Combination With Other Anti-Cancer Agents, in Solid Tumors With PIK3CA / AKT / PTEN Mutations.
[2]. ArQule Presents Recent Data on ARQ 751 at the 2019 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics.
[3]. Abstract A034: The use of biomarkers and ctDNA in a phase 1 trial of ARQ 751
[4]. Abstract 374: In vitro and in vivo anti-tumor activity of ARQ 751, a potent and selective AKT inhibitor
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 | 6.67 mg/mL (11.37 mM) | requires sonication and warming and heat to 60°C; 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 | ≥ 0.67 mg/mL (1.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (6.7 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 | ≥ 0.67 mg/mL (1.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (6.7 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 | ≥ 0.67 mg/mL (1.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 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 (6.7 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Vevorisertib shows Kd values of 1.2 nM for wild-type AKT1 and 8.6 nM for mutant AKT1-E17K, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K[4].
In Vivo
In an AKT1-E17K mutant endometrial patient-derived xenograft (PDX) model, Vevorisertib (10~120 mg/kg) exerts dose-dependent anti-tumor activity. Vevorisertib has a plasma half-life of 4 to 5 hours and shows no tissue accumulation[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
NRG1/PDGFC loop between fibroblasts and cancer cells drives paclitaxel resistance via ferroptosis suppression in breast cancer. Cell Death Discov 2025 Nov 10;11(1):520. PMID: 41213930
bioRxiv. 2026 Apr 9.
