产品
编 号：F762963
分子式：C36H49ClFN7O4
分子量：698.27
分子式：C36H49ClFN7O4
分子量：698.27
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CAS No: 3031784-60-5
产品详情
生物活性：
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
体内研究：
G4/HDAC-IN-1 (2.5 mg/kg; i.p. once daily for 31 days) shows antitumor activity.Animal Model:Five week-old female BALB/C mice with TNBC xenografts
Dosage:2.5 mg/kg
Administration:Intraperitoneal injection; 2.5 mg/kg once daily; for 31 days
Result:Showed well tolerance in vivo and exhibited potent antitumor activity.
体外研究：
G4/HDAC-IN-1 (0-10 μM; 1.5 h) shows HDAC inhibitory activity with an IC50 of 1.9 μM by determining nuclear extract and exhibits inhibitory activity on intracellular HDAC activity in MDA-MB-231 cells with an IC50 value of 1.1 μM.G4/HDAC-IN-1 (0-50 μM) shows G4 binding activity with an IC50 of 0.4 μM.G4/HDAC-IN-1 (0-10 μM; 1.5 h) inhibits HDAC1, HDAC8, HDAC4, HDAC6 and HDAC11 activities with IC50s of 1.26, 0.03, 2.64, 0.65 and 1.38 μM, respectively.G4/HDAC-IN-1 (0-50 μM) binds with Pu22, HRAS and HTG21 sequences with KD values of 1.8, 3.6 and ＞10 μM, respectively.G4/HDAC-IN-1 (1.25-5.0 μM; 48 h) dose-dependently increases DNA G4 level.G4/HDAC-IN-1 (0-50 μM; overnight) inhibits cytotoxic activities of TNBC cell lines.
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
体内研究：
G4/HDAC-IN-1 (2.5 mg/kg; i.p. once daily for 31 days) shows antitumor activity.Animal Model:Five week-old female BALB/C mice with TNBC xenografts
Dosage:2.5 mg/kg
Administration:Intraperitoneal injection; 2.5 mg/kg once daily; for 31 days
Result:Showed well tolerance in vivo and exhibited potent antitumor activity.
体外研究：
G4/HDAC-IN-1 (0-10 μM; 1.5 h) shows HDAC inhibitory activity with an IC50 of 1.9 μM by determining nuclear extract and exhibits inhibitory activity on intracellular HDAC activity in MDA-MB-231 cells with an IC50 value of 1.1 μM.G4/HDAC-IN-1 (0-50 μM) shows G4 binding activity with an IC50 of 0.4 μM.G4/HDAC-IN-1 (0-10 μM; 1.5 h) inhibits HDAC1, HDAC8, HDAC4, HDAC6 and HDAC11 activities with IC50s of 1.26, 0.03, 2.64, 0.65 and 1.38 μM, respectively.G4/HDAC-IN-1 (0-50 μM) binds with Pu22, HRAS and HTG21 sequences with KD values of 1.8, 3.6 and ＞10 μM, respectively.G4/HDAC-IN-1 (1.25-5.0 μM; 48 h) dose-dependently increases DNA G4 level.G4/HDAC-IN-1 (0-50 μM; overnight) inhibits cytotoxic activities of TNBC cell lines.
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