Tivumecirnon

Tivumecirnon (FLX475) is an orally active, selective CCR4 antagonist. Tivumecirnon blocks the binding of CCR4 to its ligands, CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. Tivumecirnon has antitumor activity[1][2][3][4].

Product Specifications

CAS Number

[2174938-78-2]

Product Name Alternative

FLX475

UNSPSC

12352005

Target

CCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/tivumecirnon.html

Purity

99.48

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C24H27Cl2F3N6O

Molecular Weight

543.41

References & Citations

[1]Hilary Plake BECK, et al. Chemokine receptor modulators and uses thereof. WO2018022992.|[2]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.|[3]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.|[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.