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编 号：F749889
分子式：C27H29NO5
分子量：447.52
分子式：C27H29NO5
分子量：447.52
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CAS No: 2217671-64-0
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生物活性：
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
体内研究：
MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 3 weeks) shows a good tolerability and antitumor activity (TGI=61%).MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 6 weeks) shows an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.MIR002 ( 50 mg/kg, twice a day for 5 days) induces a significant increase of a interferon at its pharmacological active dose (50 mg/kg).Animal Model:Model: 4-6 weeks old female CD-1 nude mice (NSCLC NCI-H460 model)
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days a week, 3 weeks
Result:Showed a good tolerability and antitumor activity (TGI=61%).
Animal Model:4-6 weeks old female CD-1 nude mice ( MM473-luc and MM487-Luc)
Dosage:50 mg/kg combibnated with cisplatin (i.p.; 5 mg/kg; twice a day for 7 days a week, 6 weeks)
Administration:p.o.; twice a day for 5 days a week, 6 weeks
Result:Showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.
Animal Model:4-6 weeks old female CD-1 nude mice (Melanoma B16 model)
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days
Result:Induced a significant increase of α interferon at its pharmacological active dose (50 mg/kg).
体外研究：
MIR002 (24 h) shows antiproliferative activity at nanomolar concentrations (IC50s of 0.25, 2.8, 0.6, 0.41 μM in NCI-H460, H460-R9A, A2780, A2780-DX; IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 μM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively).MIR002 (0.0001,0.01, 1, 10 μM) shows inhibitory activity on HDAC11 with an IC50 of 6.09 μM. MIR002 (0.1, 0.25, 0.4 μM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation.MIR002 (72 h) leads to cell cycle arrest at the G1-S phase.
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
体内研究：
MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 3 weeks) shows a good tolerability and antitumor activity (TGI=61%).MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 6 weeks) shows an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.MIR002 ( 50 mg/kg, twice a day for 5 days) induces a significant increase of a interferon at its pharmacological active dose (50 mg/kg).Animal Model:Model: 4-6 weeks old female CD-1 nude mice (NSCLC NCI-H460 model)
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days a week, 3 weeks
Result:Showed a good tolerability and antitumor activity (TGI=61%).
Animal Model:4-6 weeks old female CD-1 nude mice ( MM473-luc and MM487-Luc)
Dosage:50 mg/kg combibnated with cisplatin (i.p.; 5 mg/kg; twice a day for 7 days a week, 6 weeks)
Administration:p.o.; twice a day for 5 days a week, 6 weeks
Result:Showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.
Animal Model:4-6 weeks old female CD-1 nude mice (Melanoma B16 model)
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days
Result:Induced a significant increase of α interferon at its pharmacological active dose (50 mg/kg).
体外研究：
MIR002 (24 h) shows antiproliferative activity at nanomolar concentrations (IC50s of 0.25, 2.8, 0.6, 0.41 μM in NCI-H460, H460-R9A, A2780, A2780-DX; IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 μM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively).MIR002 (0.0001,0.01, 1, 10 μM) shows inhibitory activity on HDAC11 with an IC50 of 6.09 μM. MIR002 (0.1, 0.25, 0.4 μM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation.MIR002 (72 h) leads to cell cycle arrest at the G1-S phase.
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