Home Immunology & Inflammation CXCR inhibitor SX-682 For research use only.

SX-682

SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity.

SX-682 Chemical Structure

SX-682 Chemical Structure

CAS: 1648843-04-2

Selleck's SX-682 has been cited by 1 publication

Purity & Quality Control

Batch: S894701 DMSO] 93 mg/mL] false] Ethanol] 93 mg/mL] false] Water] ˂1 mg/mL] false Purity: 98.66%
98.66

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Signaling Pathway

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Biological Activity

Description SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity.
Targets
CXCR1 [2] CXCR2 [2]
In Vivo
In vivo

Whole tumor accumulation of CXCL1 in vivo in MOC1 and LLC tumors is significantly greater than oral mucosa and normal lung, respectively, and not diminished with SX-682 treatment. Plasma accumulation of CXCL1 is greater in tumor-bearing mice compared with naive for both models and increases following SX-682 treatment. Treatment of mice bearing MOC1 or LLC tumors with SX-682 beginning 10 or 20 days after tumor initiation does not alter CXCR1 or CXCR2 expression on tumor cells in vivo.[2] Following in vivo SX-682 treatment, tumor PMN-MDSC expression of cell surface TGF-β or superoxide dismutase 1/2 genes, responsible for the generation of H2O2, is not significantly altered.[3]
Animal Research Animal Models wild-type C57BL/6 mice subcutaneously injected with MOC2 cells (1x105 cells in PBS)
Dosages 500 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04245397 Recruiting
Myelodysplastic Syndromes
Syntrix Biosystems Inc.|H. Lee Moffitt Cancer Center and Research Institute|National Heart Lung and Blood Institute (NHLBI)|Johns Hopkins University|AdventHealth|Emory University|University of Miami|Mayo Clinic
 May 12 2020 Phase 1
NCT03161431 Recruiting
Melanoma Stage III|Melanoma Stage IV
Syntrix Biosystems Inc.|Massachusetts General Hospital|National Cancer Institute (NCI)|Dana-Farber Cancer Institute|Mayo Clinic|University of Rochester|M.D. Anderson Cancer Center|University of Miami
 June 12 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 467.20 Formula

C19H14BF4N3O4S
CAS No. 1648843-04-2 SDF --
Smiles B(C1=C(C=C(C=C1)OC(F)(F)F)CSC2=NC=C(C=N2)C(=O)NC3=CC=C(C=C3)F)(O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 93 mg/mL ( (199.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 93 mg/mL

Water : ˂1 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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