产品
编 号：F762809
分子式：C25H18BrFN6O3
分子量：549.35
分子式：C25H18BrFN6O3
分子量：549.35
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CAS No: 3032451-66-1
产品详情
生物活性：
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.
体内研究：
YCH1899 (5 mg/kg, 静脉给药) 在大鼠中具有中等清除力。 YCH1899在MDA-MB-436/OP (6.25, 12.5和25 mg/kg, 口服给药，每天一次，持续27天) 和Capan-1/R（12.5和25 mg/kg, 口服给药，每天一次，持续21天） 异种移植小鼠肿瘤模型中克服了Talazoparib耐药，肿瘤体积显著下降。Animal Model:MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice
Dosage:12.5 and 25 mg/kg
Administration:Oral administration
Result:Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kgInhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.
Animal Model:rats
Dosage:5 mg/kg
Administration:Intravenous injection
Result:Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
体外研究：
YCH1899 (7天) 对Capan-1、Capan-1/OP、Capan-1/TP 细胞表现出明显的抗增殖活性，IC50 分别为0.10、0.89、1.13 nM。YCH1899 (0.001-1 nM, 4 h) 稳定PARP1-DNA复合物，抑制PARP的形成。YCH1899 (3.5 h) 对BRCA突变/野生型细胞 (V?C8, V79, HCT-15, HCC1937) 的增殖有抑制作用, IC50s 范围为1.19-44.24 nM。YCH1899 (1 μM, 24 h) 在 Capan-1、Capan-1/OP、Capan-1/TP 细胞中诱导 DNA 损伤，使 γH2AX 数量大量增加。YCH1899 (1 μM, 48 h) 在 U2OS-DR-GFP 细胞中诱导 HR (Homologous Recombination, 同源重组) 修复活性显著降低。
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.
体内研究：
YCH1899 (5 mg/kg, 静脉给药) 在大鼠中具有中等清除力。 YCH1899在MDA-MB-436/OP (6.25, 12.5和25 mg/kg, 口服给药，每天一次，持续27天) 和Capan-1/R（12.5和25 mg/kg, 口服给药，每天一次，持续21天） 异种移植小鼠肿瘤模型中克服了Talazoparib耐药，肿瘤体积显著下降。Animal Model:MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice
Dosage:12.5 and 25 mg/kg
Administration:Oral administration
Result:Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kgInhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.
Animal Model:rats
Dosage:5 mg/kg
Administration:Intravenous injection
Result:Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
体外研究：
YCH1899 (7天) 对Capan-1、Capan-1/OP、Capan-1/TP 细胞表现出明显的抗增殖活性，IC50 分别为0.10、0.89、1.13 nM。YCH1899 (0.001-1 nM, 4 h) 稳定PARP1-DNA复合物，抑制PARP的形成。YCH1899 (3.5 h) 对BRCA突变/野生型细胞 (V?C8, V79, HCT-15, HCC1937) 的增殖有抑制作用, IC50s 范围为1.19-44.24 nM。YCH1899 (1 μM, 24 h) 在 Capan-1、Capan-1/OP、Capan-1/TP 细胞中诱导 DNA 损伤，使 γH2AX 数量大量增加。YCH1899 (1 μM, 48 h) 在 U2OS-DR-GFP 细胞中诱导 HR (Homologous Recombination, 同源重组) 修复活性显著降低。
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