产品
编 号：F235577
分子式：C18H24Cl2N6O
分子量：411.33
分子式：C18H24Cl2N6O
分子量：411.33
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1883545-60-5
产品详情
生物活性：
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7?nM. CRT0066101 dihydrochloride has anticancer effects.
体内研究：
CRT0066101（80 mg/kg/天；口服灌胃；每天一次；持续 21 天）dihydrochloride 在 Panc-1 原位模型中可有效阻止体内肿瘤生长。Animal Model:CR-UK nu/nu mice injected with Panc-1 cells
Dosage:80 mg/kg/day
Administration:Oral gavage; once daily; for 21 days
Result:Potently blocked tumor growth in vivo.
体外研究：
CRT0066101 (5 μM; 1 h) dihydrochloride 可阻断 Panc-1 和 Panc-28 细胞中基础和 NT 诱导的 pS916-PKD1/2（激活的 PKD1/2）。CRT0066101 dihydrochloride 消除 NT 诱导的 Hsp27 (pS82-Hsp27) 磷酸化，减弱 PKD1 介导的 NF-κB 激活，并消除 NF-κB 依赖性增殖和促生存蛋白的表达 .CRT0066101 dihydrochloride 显着抑制 Panc-1 细胞增殖，IC50 值为 1 μM。CRT0066101 dihydrochloride 可诱导 Panc-1 细胞凋亡 6-10 倍。CRT0066101 dihydrochloride 显着降低 Colo357、Panc-1、MiaPaCa-2 和 AsPC-1 细胞的增殖，但对 Capan-2 细胞有一定影响。
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7?nM. CRT0066101 dihydrochloride has anticancer effects.
体内研究：
CRT0066101（80 mg/kg/天；口服灌胃；每天一次；持续 21 天）dihydrochloride 在 Panc-1 原位模型中可有效阻止体内肿瘤生长。Animal Model:CR-UK nu/nu mice injected with Panc-1 cells
Dosage:80 mg/kg/day
Administration:Oral gavage; once daily; for 21 days
Result:Potently blocked tumor growth in vivo.
体外研究：
CRT0066101 (5 μM; 1 h) dihydrochloride 可阻断 Panc-1 和 Panc-28 细胞中基础和 NT 诱导的 pS916-PKD1/2（激活的 PKD1/2）。CRT0066101 dihydrochloride 消除 NT 诱导的 Hsp27 (pS82-Hsp27) 磷酸化，减弱 PKD1 介导的 NF-κB 激活，并消除 NF-κB 依赖性增殖和促生存蛋白的表达 .CRT0066101 dihydrochloride 显着抑制 Panc-1 细胞增殖，IC50 值为 1 μM。CRT0066101 dihydrochloride 可诱导 Panc-1 细胞凋亡 6-10 倍。CRT0066101 dihydrochloride 显着降低 Colo357、Panc-1、MiaPaCa-2 和 AsPC-1 细胞的增殖，但对 Capan-2 细胞有一定影响。
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