SX-682 | CXCR1/2 inhibitor

CAS:
1648843-04-2
Catalog Number:
10-4925
Activity:
CXCR1/2 inhibitor
Chemical Names:
[2-[[5-[(4-Fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid
Molecular Weight:
467.20
Molecular Formula:
C19H14BF4N3O4S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$90.00
25 mg$280.00

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:

  1. Zebala et al. (2015), WO2015/016938
  2. Lu et al. (2017), Effective combinatorial immunotherapy for castration-resistant prostate cancer; Nature 542 728
  3. Kargl et al. (2019), Neutrophil content predicts lymphocyte depletion and anti-PD1 treatment failure in NSCLC; JCI Insight 4 e130850
  4. Sun et al. (2019), Inhibiting myeloid-derived suppressor cell trafficking enhances T cell immunotherapy; JCI Insight 4 e126853
  5. 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
CAS:
1648843-04-2
Catalog Number:
10-4925
Activity:
CXCR1/2 inhibitor
Chemical Names:
[2-[[5-[(4-Fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid
Molecular Weight:
467.20
Molecular Formula:
C19H14BF4N3O4S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee