[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid manufacturers
- SX-682
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- $34.00 / 1mg
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2025-05-14
- CAS:1648843-04-2
- Min. Order:
- Purity: 99.57%
- Supply Ability: 10g
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| | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Basic information |
| Product Name: | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid | | Synonyms: | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid;SX-682;Boronic acid, B-[2-[[[5-[[(4-fluorophenyl)amino]carbonyl]-2-pyrimidinyl]thio]methyl]-4-(trifluoromethoxy)phenyl]-;(2-(((5-((4-fluorophenyl)carbamoyl)pyrimidin-2-yl)thio)methyl)-4-(trifluoromethoxy)phenyl)boronic acid;cells,SX-682,allosteric,SX 682,recruitment,suppressor,Inhibitor,tumor,CXCR,CXC chemokine receptors,SX682,immunity,MDSCs,inhibit,myeloid-derived,antitumor;2-[[[5-[(4-Fluorophenyl)carbamoyl]-2-pyrimidinyl]thio]methyl]-4-(trifluoromethoxy)phenylboronic Acid;SX-682, 10 mM in DMSO | | CAS: | 1648843-04-2 | | MF: | C19H14BF4N3O4S | | MW: | 467.2 | | EINECS: | 604-604-1 | | Product Categories: | | | Mol File: | 1648843-04-2.mol | ![[2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Structure](CAS/20200119/GIF/1648843-04-2.gif) |
| | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Chemical Properties |
| 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. |
| | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Usage And Synthesis |
| 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 | | Uses | SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity[1]. | | in vivo | SX-682 (50 mg/kg; orally; twice a day on a Monday through Friday) has Meager to moderate effects as single agents on CRPC progression was observed, yet combination with ICB produced strong efficacy[2]. | Animal Model: | C57BL/6NTac-Tyrtm1Arte?female mice[2] | | Dosage: | 50 mg/kg | | Administration: | Orally; twice a day on a Monday through Friday | | Result: | Has Meager to moderate effects on CRPC progression. |
| | IC 50 | CXCR1; CXCR2 | | 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 |
| | [2-[[5-[(4-fluorophenyl)carbamoyl]pyrimidin-2-yl]sulfanylmethyl]-4-(trifluoromethoxy)phenyl]boronic acid Preparation Products And Raw materials |
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