| Field | Specification |
|---|---|
| Target | |
| Alternative names | FLX475 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H27Cl2F3N6O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Tivumecirnon, also known as FLX475, is an orally active, selective antagonist of CCR4 that blocks the binding of CCR4 to its ligands CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. It has shown antitumor activity[1][2][3][4]. It is supplied as an off-white to light yellow solid (C24H27Cl2F3N6O, MW 543.41) at 99.48% purity.
Physical & Chemical Properties
| CAS Number | 2174938-78-2 |
|---|---|
| Molecular Formula | C24H27Cl2F3N6O |
| Molecular Weight | 543.41 g/mol |
| Purity | 99.48% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | C[C@H](C1=C(C=C(C=C1)Cl)Cl)N2C3=NC(N4CC([C@H]5CCCN(C5)CCO)C4)=CN=C3C(C(F)(F)F)=N2 |
| Target | CCR4 |
| Signaling Pathway | GPCR/G Protein; Immunology/Inflammation |
| Solubility | In Vitro: DMSO: 100 mg/mL (184.02 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.
[1]. Tae Min Kim, et al. 629-C Phase 2 safety and efficacy of oral CCR4 antagonist FLX475 (tivumecirnon) plus pembrolizumab in subjects with non-small cell lung cancer not previously treated with checkpoint inhibitor[J]. 2023.
[2]. Hilary Plake BECK, et al. Chemokine receptor modulators and uses thereof. WO2018022992.
[3]. Adam Grant, et al. Abstract 2485: A combined mregDC and Treg signature associates with antitumor efficacy of CCR4 antagonist tivumecirnon FLX475. Cancer Res 15 March 2024; 84 (6_Supplement): 2485.
[4]. Dirk G. Brockstedt, et al., Clinical and biological activity of FLX475, an oral CCR4 antagonist, in advanced cancer. Journal of Clinical Oncology. 2023. 41, 2625-2625.
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 (184.02 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 + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.60 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 Vitro
Tivumecirnon is applied together with Pembrolizumab in treating non-small cell lung cancer[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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