产品
编 号:F522682
分子式:C5H6BrN3O5
分子量:268.02
产品类型
结构图
CAS No: 925206-65-1
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产品详情
生物活性:
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
体内研究:
RRx-001 (5 mg/kg 或 10 mg/kg,静脉注射,每周三次,持续 24 天) 在异种移植小鼠模型中抑制肿瘤生长并延长存活期。 RRx-001 (10 mg/kg,IP,每周两次和每天一次) 对 A549 肺癌模型表现出有效的抗癌活性,这取决于肿瘤组织中是否存在肿瘤相关巨噬细胞 (TAM)。Animal Model:CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 106 MM.1S cells in 100 μL of serum-free RPMI 1640 medium.
Dosage:5 mg/kg or 10 mg/kg.
Administration:I.V., thrice-weekly for 24 days.
Result:Blocked MM tumor growth and enhances survival. Treatment was well tolerated, suggested by no apparent weight loss.
Animal Model:Female BALB/c nude mice (19.2?±?1.7?g) based on A549 lung cancer model.
Dosage:10?mg/kg.
Administration:IP, twice a week and once a day.
Result:Resulted in the most significant tumor growth retardation.Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.
体外研究:
RRx-001 (0-5 μM,24 小时) 抑制 MM 细胞生长并克服对新型和常规疗法的耐药性。RRx-001 阻断 MM 细胞的迁移和相关的血管生成。RRx-001 诱导显著的 G1 期生长停滞,并伴随 S 期减少。RRx-001 引发 MM 细胞显著凋亡。RRx-001 通过下调DNA甲基转移酶抑制DNA甲基化。RRx-001 和 RRx-001 处理的巨噬细胞上清液下调肿瘤细胞上的 CD47 和巨噬细胞上的 SIRPα。