2174938-78-2
Chemical Structure
Tivumecirnon
Synonym(s): FLX475
- CAS No.: 2174938-78-2
- Formula:C24H27Cl2F3N6O
- Molecular Weight:543.41
IUPAC Name: 2-((R)-3-(1-(1-((R)-1-(2,4-dichlorophenyl)ethyl)-3-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)azetidin-3-yl)piperidin-1-yl)ethan-1-ol
InChIKey: AKSVALRPYDVQBS-CABCVRRESA-N
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
Biological Activity: 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].
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Tivumecirnon | 99.48% | 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. | ||||||||||||||||||||
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- [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.
Keywords
