产品
编 号：F287236
分子式：C50H62ClN11O6S2
分子量：1012.68
分子式：C50H62ClN11O6S2
分子量：1012.68
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2376047-73-1
产品详情
生物活性：
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
体内研究：
SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively. Animal Model:NOD/SCID mice with termed K562-Luc
Dosage:5, 15, and 45 mg/kg
Administration:Ip; 12 days
Result:Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.
Animal Model:Female Wistar rats
Dosage:2 mg/kg (Pharmacokinetic Analysis)
Administration:Iv or ip; 24 hours
Result:Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.
体外研究：
SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner.SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5.SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
体内研究：
SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively. Animal Model:NOD/SCID mice with termed K562-Luc
Dosage:5, 15, and 45 mg/kg
Administration:Ip; 12 days
Result:Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.
Animal Model:Female Wistar rats
Dosage:2 mg/kg (Pharmacokinetic Analysis)
Administration:Iv or ip; 24 hours
Result:Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.
体外研究：
SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner.SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5.SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.
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