| Identification | Back Directory | [Name]
[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid | [CAS]
1648843-04-2 | [Synonyms]
SX-682
[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid
Boronic acid, B-[2-[[[5-[[(4-fluorophenyl)amino]carbonyl]-2-pyrimidinyl]thio]methyl]-4-(trifluoromethoxy)phenyl]- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H14BF4N3O4S | [MDL Number]
MFCD28502254 | [MOL File]
1648843-04-2.mol | [Molecular Weight]
467.2 |
| Chemical Properties | Back Directory | [density ]
1.53±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
8.18±0.53(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
SX-682 is a novel CXCR1/2 inhibitor (IC50s: CXCR1 = 42 nM, CXCR2 = 20 nM).1?It displayed robust synergistic activity with immune checkpoint blockade against castration resistant prostate cancer.2 It significantly reduced tumor burden in a Ptenfl/fl/Lkb1fl/fl mouse model of lung squamous cell cancer when used in combination with anti-PD1 therapy.3 SX-682 significantly inhibited trafficking of neutrophilic myeloid-derived suppressor cells (PMN-MDSCs) enhancing anti-PD1 immune checkpoint blockade, T cell-based immunotherapy, and NK-cell immunotherapy.4,5 | [Uses]
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity[1]. | [in vivo]
SX-682 (50 mg/kg; orally; twice a day on a Monday through Friday) has Meager to moderate effects as single agents on CRPC progression was observed, yet combination with ICB produced strong efficacy[2]. | Animal Model: | C57BL/6NTac-Tyrtm1Arte?female mice[2] | | Dosage: | 50 mg/kg | | Administration: | Orally; twice a day on a Monday through Friday | | Result: | Has Meager to moderate effects on CRPC progression. |
| [IC 50]
CXCR1; CXCR2 | [storage]
Store at -20°C | [References]
Zebala et al. (2015), WO2015/016938
Lu et al. (2017), Effective combinatorial immunotherapy for castration-resistant prostate cancer; Nature 542 728
Kargl et al. (2019), Neutrophil content predicts lymphocyte depletion and anti-PD1 treatment failure in NSCLC; JCI Insight 4 e130850
Sun et al. (2019), Inhibiting myeloid-derived suppressor cell trafficking enhances T cell immunotherapy; JCI Insight 4 e126853
Greene et al. (2020), Inhibition of MDSC Trafficking with SX-682, a CXCR1/2 Inhibitor, Enhances NK-Cell Immunotherapy in Head and Neck Cancer Models; Clin. Cancer Res. 26 1420 |
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