SX-682 是口服有效的CXCR1和CXCR2变构抑制剂,可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫,具有治疗去势抵抗性前列腺癌的潜力。 Information 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. Targets CXCR1 ; CXCR2 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 H 2 O 2 , is not significantly altered. [3]
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SX-682
Dangerous GoodsCAS number:1648843-04-2 molecular formula:C19H14BF4N3O4S
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | (2-(((5-((4-Fluorophenyl)carbamoyl)pyrimidin-2-yl)thio)methyl)-4-(trifluoromethoxy)phenyl)boronicacid | GTPL10165 | AKOS040759427 | EX-A4295 | AC-36549 | SB17394 | H5212R2DPM | 1648843-04-2 | BCP32154 | (2-(((5-((4-Fluorophenyl)carbamoyl)pyrimidin-2-yl)th | ||
| CAS number | 1648843-04-2 | molecular formula | C19H14BF4N3O4S |
| molecular weight | 467.2 g/mol | Exact mass | - |
| PSA | 130.000 Ų | logp | 5.761 |
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Safety information
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。
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