| Field | Specification |
|---|---|
| Alternative names | CRX-601 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C81H157N2O16P |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK1795091, also known as CRX-601, is an immunologic stimulator and synthetic TLR4 agonist with antitumor activity. It can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines, and in mouse models it inhibits tumor growth and increases survival, as well as producing long-term survival in an influenza challenge model[1][2][3]. It is supplied as a white to off-white solid (C81H157N2O16P, MW 1446.09) at 94.48% purity.
Physical & Chemical Properties
| CAS Number | 1233589-81-5 |
|---|---|
| Molecular Formula | C81H157N2O16P |
| Molecular Weight | 1446.09 g/mol |
| Purity | 94.48% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)O[C@@H]([C@@H]([C@H]1CO)O[P](O)(O)=O)[C@H]([C@@H](O1)OC[C@@H](C(O)=O)NC(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)=O)NC(C[C@H](OCCCCCCCCCC)CCCCCCCCCCC)=O |
| Signaling Pathway | Immunology/Inflammation |
| Solubility | In Vitro: DMSO: 25 mg/mL (17.29 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. 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 | 25 mg/mL (17.29 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 (1.73 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). 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% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (1.73 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 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 (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
Given intranasally at 0.1 μg/mouse, GSK1795091 (CRX-601) serves as an adjuvant with detergent split-influenza antigen (H3N2) and elicits strong mucosal as well as systemic immune responses in mice[2]. In a mouse tumor model, GSK1795091 (25 μg/mouse; iv; once weekly for 3 doses) suppresses tumor growth and yields long term survival[3].
| Animal Model | Female BALB/c mice primed with H3N2[1] |
|---|---|
| Dosage | 0.1 μg /mouse |
| Administration | Intranasal administration |
| Result | As an adjuvant combined with detergent split-influenza antigen (H3N2) generated strong local and systemic immunity against co-administered influenza antigens while exhibiting high efficacy against two heterotypic influenza challenges. Mice receiving adjuvanted vaccines had significantly higher IgA titers than non-adjuvanted (vehicle) controls in an adjuvant dose-dependent manner. Adjuvanted vaccines promoted antigen-specific IgG and IgA antibody responses and the generation of polyfunctional antigen-specific Th17 cells. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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