[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Property

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 and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Chemical Properties,Usage,Production

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

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