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编 号：F754377
分子式：C42H54N12O5
分子量：806.96
分子式：C42H54N12O5
分子量：806.96
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CAS No: 2649400-34-8
产品详情
生物活性：
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker).
体内研究：
NX-5948 (BTK-IN-24；10、30 mg/kg；口服灌胃；每日；第 18 至 36 天) 在小鼠胶原诱导的关节炎 (CIA) 模型中有效且耐受性良好，可抑制抗体滴度和细胞因子 IL-6 水平。NX-5948 (3、10、30 mg/kg；口服灌胃) 会导致小鼠和非人灵长类、食蟹猴 B 细胞循环中 BTK 水平呈剂量和时间依赖性降低。Animal Model:Mouse collagen-induced arthritis (CIA) model
Dosage:10, 30 mg/kg
Administration:PO; daily; Day 18 to 36
Result:Showed efficacious and well-tolerated in a mouse CIA model.
体外研究：
NX-5948 (BTK-IN-24；0.0001-1000 nM；4 小时) 是原代人 B 细胞中 BTK 的有效降解剂 (DC50=0.34 nM)，抑制 BCR 信号传导。NX-5948 在淋巴瘤细胞系和 PBMC 中诱导 BTK 降解 (DC50NX-5948 相关抗体:
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker).
体内研究：
NX-5948 (BTK-IN-24；10、30 mg/kg；口服灌胃；每日；第 18 至 36 天) 在小鼠胶原诱导的关节炎 (CIA) 模型中有效且耐受性良好，可抑制抗体滴度和细胞因子 IL-6 水平。NX-5948 (3、10、30 mg/kg；口服灌胃) 会导致小鼠和非人灵长类、食蟹猴 B 细胞循环中 BTK 水平呈剂量和时间依赖性降低。Animal Model:Mouse collagen-induced arthritis (CIA) model
Dosage:10, 30 mg/kg
Administration:PO; daily; Day 18 to 36
Result:Showed efficacious and well-tolerated in a mouse CIA model.
体外研究：
NX-5948 (BTK-IN-24；0.0001-1000 nM；4 小时) 是原代人 B 细胞中 BTK 的有效降解剂 (DC50=0.34 nM)，抑制 BCR 信号传导。NX-5948 在淋巴瘤细胞系和 PBMC 中诱导 BTK 降解 (DC50NX-5948 相关抗体:
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