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TargetMol - Model SX-682 -Allosteric Inhibitor
SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.
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- Targets&IC50: CXCR2:20 nM, CXCR1:42 nM
- In vitro: SX-682 significantly inhibits PMN-MDSC trafficking without altering CXCR2 ligand expression; combination with SX-682 enhances tumor growth inhibition or established tumor rejection following programmed death axis (PD-axis) immune checkpoint blockade or adoptive cell transfer of engineered T cells; CXCR1/2 are expressed on tumor cells, but SX-682 appears to have little direct antitumor effect on these cancer cells. [1]
- In vivo: METHODS: SX-682 (500 mg/kg, oral, one week) was used to treat tumor suppressor model mice injected subcutaneously with MOC2 cells, and PMN-MDSC accumulation was evaluated by flow cytometry.
- RESULTS SX-682 significantly reduced PMN-MDSC trafficking into MOC2 tumors, but SX-682 treatment did not alter the proliferation of tumor PMN-MDSC in tumor-bearing mice. The main mechanism of SX-682 is to inhibit PMN-MDSC trafficking into MOC2 tumors. [2]
- Molecular Weight: 467.2
- Formula: C19H14BF4N3O4S
- Cas No.: 1648843-04-2
- Smiles: C(SC=1N=CC(C(NC2=CC=C(F)C=C2)=O)=CN1)C3=C(B(O)O)C=CC(OC(F)(F)F)=C3
- Relative Density.: 1.53 g/cm3 (Predicted)