产品
编 号：F741534
分子式：C39H49N9O5S
分子量：755.93
分子式：C39H49N9O5S
分子量：755.93
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2380274-50-8
产品详情
生物活性：
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
体内研究：
AU-15330 (10 和 30 mg/kg；静脉注射；每周 5 天，持续 3 周) 在免疫活性小鼠中未显示明显毒性。 AU-15330 (60 mg/kg 含或不含 10 mg/kg 恩杂鲁胺；静脉注射；每周 3 天；口服；每周 5 天，持续 5 周) 可有效抑制肿瘤生长，在超过 20% 的动物中引发疾病消退。组合方案诱导最有效的抗肿瘤作用，所有动物均出现消退。 AU-15330 (60 mg/kg，含或不含 10 mg/kg 恩杂鲁胺；iv；每周 3 天；口服；每周 5 天，持续 5 周) 作为单一药物并与恩杂鲁胺协同作用，强烈抑制 C4-2B 细胞系衍生的 CRPC 异种移植物在完整小鼠中的生长。 AU-15330 (60 mg/kg 含或不含 10 mg/kg enzalutamide；iv；每周 3 天；口服每周 5 天，共 5 周) 与 enzalutamide 联合使用可显著抑制肿瘤生长，在超过 30% 的动物中导致肿瘤消退，MDA-PCa-146-12 PDX 的 CRPC 变体模型通过肿瘤植入阉割小鼠。Animal Model:Six-week-old male CB17 severe combined immunodeficiency (SCID) mice
Dosage:10 and 30 mg/kg
Administration:i.v. (5 days per week for 3 weeks)
Result:Showed no evident toxicity in immuno-competent mice.
Animal Model:VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:60 mg/kg with or without 10?mg/kg enzalutamide
Administration:i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
Result:Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
Animal Model:C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:60 mg/kg with or without 30?mg/kg enzalutamide
Administration:i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
Result:Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
体内研究：
AU-15330 (10 和 30 mg/kg；静脉注射；每周 5 天，持续 3 周) 在免疫活性小鼠中未显示明显毒性。 AU-15330 (60 mg/kg 含或不含 10 mg/kg 恩杂鲁胺；静脉注射；每周 3 天；口服；每周 5 天，持续 5 周) 可有效抑制肿瘤生长，在超过 20% 的动物中引发疾病消退。组合方案诱导最有效的抗肿瘤作用，所有动物均出现消退。 AU-15330 (60 mg/kg，含或不含 10 mg/kg 恩杂鲁胺；iv；每周 3 天；口服；每周 5 天，持续 5 周) 作为单一药物并与恩杂鲁胺协同作用，强烈抑制 C4-2B 细胞系衍生的 CRPC 异种移植物在完整小鼠中的生长。 AU-15330 (60 mg/kg 含或不含 10 mg/kg enzalutamide；iv；每周 3 天；口服每周 5 天，共 5 周) 与 enzalutamide 联合使用可显著抑制肿瘤生长，在超过 30% 的动物中导致肿瘤消退，MDA-PCa-146-12 PDX 的 CRPC 变体模型通过肿瘤植入阉割小鼠。Animal Model:Six-week-old male CB17 severe combined immunodeficiency (SCID) mice
Dosage:10 and 30 mg/kg
Administration:i.v. (5 days per week for 3 weeks)
Result:Showed no evident toxicity in immuno-competent mice.
Animal Model:VCaP castration-resistant tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:60 mg/kg with or without 10?mg/kg enzalutamide
Administration:i.v. (3 days per week); p.o. (5 days per week for 5 weeks)
Result:Resulted inhibition of tumor growth and triggered disease regression in more than 20% of animals. Combinatorial regimen induced the most potent anti-tumour effect, with regression in all animals.
Animal Model:C4-2B non-castrated tumour model (six-week-old male CB17 severe combined immunodeficiency (SCID) mice)
Dosage:60 mg/kg with or without 30?mg/kg enzalutamide
Administration:i.v. (3 days per week); p.o. (5 days per week for 4 weeks)
Result:Strongly inhibited the growth of C4-2B cell line-derived CRPC xenografts in intact mice as a single agent and synergized with enzalutamide.
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