产品
编 号：F754417
分子式：C31H41N7O4
分子量：575.7
分子式：C31H41N7O4
分子量：575.7
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CAS No: 2653339-26-3
产品详情
生物活性：
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity.
体内研究：
HDAC-IN-50 (15、30 mg/kg；口服；每日一次，持续 18 天) 在小鼠体内显示出抗肿瘤活性。Animal Model:BALB/c nude mice (HCT116 xenograft model)
Dosage:15, 30 mg/kg
Administration:P.o.; daily for 18 days
Result:Inhibited the tumor growth and downregulated the expression of pSTAT3, pFGFR1, increased the expression of Ac-H3.
体外研究：
HDAC-IN-50 (compound 10e) (0.1, 1, 10, 100 nM; 12-84 h) 以时间和剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 G0/G1 期。HDAC-IN-50 (0, 1.25, 2.5, 5 μM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells; 36 h) 以剂量依赖性方式降低 pFGFR1、pERK、pSTAT3 的表达 。
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity.
体内研究：
HDAC-IN-50 (15、30 mg/kg；口服；每日一次，持续 18 天) 在小鼠体内显示出抗肿瘤活性。Animal Model:BALB/c nude mice (HCT116 xenograft model)
Dosage:15, 30 mg/kg
Administration:P.o.; daily for 18 days
Result:Inhibited the tumor growth and downregulated the expression of pSTAT3, pFGFR1, increased the expression of Ac-H3.
体外研究：
HDAC-IN-50 (compound 10e) (0.1, 1, 10, 100 nM; 12-84 h) 以时间和剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 G0/G1 期。HDAC-IN-50 (0, 1.25, 2.5, 5 μM for HCT116 cells, 0, 1, 10, 100 nM for SNU-16 cells; 36 h) 以剂量依赖性方式降低 pFGFR1、pERK、pSTAT3 的表达 。
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