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Purity: ≥98%
SX-682 (SX682) is a novel boronic acid-containing and selective CXCR2 chemokine receptor antagonist with potential anticancer and immunomodulatory activities. The proliferation and progression of tumor cells are facilitated by the upregulation of the CXC chemokine receptor CXCR2 in a range of distinct tumor cell types. Reduced tumorigenesis and metastasis were the results of CXCR2 inhibition. SX-682 is a CXCR2 antagonist that may be used to treat melanoma and prostate cancer that is resistant to castration. Syntrix Biosystems, Inc. has initiated a phase I clinical trial combining SX-682 and pembrolizumab for the treatment of metastatic melanoma.
| Targets |
CXCR2; CXCR1
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| Additional Infomation |
CXCR1/2 Inhibitor SX-682 is an orally bioavailable, selective and reversible antagonist of C-X-C motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory and antineoplastic activities. Upon administration CXCR1/2 inhibitor SX-682 selectively and allosterically binds to CXCR 1 and 2 and inhibits their activation by tumor-secreted chemokines. This inhibits CXCR1/2-mediated signaling, reduces both recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment (TME), inhibits inflammatory processes and abrogates the immunosuppressive-induced nature of the TME. This allows effector cells, such as natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer cells. This inhibits tumor cell migration, metastasis, angiogenesis and tumor cell proliferation. CXCR1 and 2, G protein-coupled receptor proteins located on myeloid cells and certain tumor cells, play key roles in the immunosuppressive nature of the TME, tumor metastasis, therapy-resistance and myeloid cell suppression. They play a key role in inflammation and their expression is elevated in several inflammatory-driven diseases.
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| Molecular Formula |
C19H14BF4N3O4S
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| Molecular Weight |
467.20
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| Exact Mass |
467.07
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| Elemental Analysis |
C, 48.85; H, 3.02; B, 2.31; F, 16.27; N, 8.99; O, 13.70; S, 6.86
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| CAS # |
1648843-04-2
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| Related CAS # |
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| PubChem CID |
90467234
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.53±0.1 g/cm3(Predicted)
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1N=CC(=CN=1)C(NC1C=CC(=CC=1)F)=O)CC1C=C(C=CC=1B(O)O)OC(F)(F)F
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| InChi Key |
SDUDZBCEHIZMFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14BF4N3O4S/c21-13-1-3-14(4-2-13)27-17(28)12-8-25-18(26-9-12)32-10-11-7-15(31-19(22,23)24)5-6-16(11)20(29)30/h1-9,29-30H,10H2,(H,27,28)
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| Chemical Name |
[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 11.76 mg/mL (25.17 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication (<60°C).
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1404 mL | 10.7021 mL | 21.4041 mL | |
| 5 mM | 0.4281 mL | 2.1404 mL | 4.2808 mL | |
| 10 mM | 0.2140 mL | 1.0702 mL | 2.1404 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04574583 | Active Recruiting |
Drug: SX-682 Drug: M7824 |
Metastatic Cancer Solid Tumors |
National Cancer Institute (NCI) |
November 24, 2020 | Phase 1 Phase 2 |
| NCT04245397 | Recruiting | Drug: Decitabine Drug: SX-682 |
Myelodysplastic Syndromes | Syntrix Biosystems, Inc. | May 12, 2020 | Phase 1 |
| NCT03161431 | Recruiting | Drug: SX-682 Biological: Pembrolizumab |
Melanoma Stage III Melanoma Stage IV |
Syntrix Biosystems, Inc. | June 12, 2019 | Phase 1 |
| NCT05604560 | Recruiting | Drug: Tislelizumab Drug: SX-682 |
Pancreatic Cancer | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins |
November 8, 2023 | Phase 2 |
| NCT04599140 | Recruiting | Drug: CXCR1/2 Inhibitor SX-682 Biological: Nivolumab |
Stage III Colon Cancer AJCC v8 Stage IV Colon Cancer AJCC v8 |
M.D. Anderson Cancer Center | October 14, 2020 | Phase 1 Phase 2 |
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