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MIR002
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MIR002图片
CAS NO:2217671-64-0
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
MIR002 是一种有效且具有口服活性的DNA polymerase α (POLA1)和HDAC 11双重抑制剂。MIR002 诱导 p53 的乙酰化、p21 的激活、G1/S 细胞周期停滞和细胞凋亡apoptosis。MIR002 显示出显著的体内抗肿瘤活性。
生物活性

MIR002 is a potent and orally activeDNA polymerase α (POLA1)andHDAC11dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, andapoptosis. MIR002 shows significant antitumor activity in vivo[1].

IC50& Target

HDAC11

6.09 μM (IC50)

POLA1

 

体外研究
(In Vitro)

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)[1].
MIR002 (0.0001,0.01, 1, 10 μM) shows inhibitory activity on HDAC11 with an IC50of 6.09 μM[1].
MIR002 (0.1, 0.25, 0.4 μM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation[1]. MIR002 (72 h) leads to cell cycle arrest at the G1-S phase[1].

Cell Proliferation Assay[1]

Cell Line:MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells
Concentration:10 scalar concentrations
Incubation Time:24 h
Result:Showed antiproliferative activity at nanomolar concentrations (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)

Western Blot Analysis[1]

Cell Line:NCI-H460, MM473, MM487, A2780 cells
Concentration:0.1, 0.25, 0.4 μM
Incubation Time:24 h
Result:Showed antiproliferative activity at nanomolar concentrations (IC50s of 0.9, 1.2, Showed a dosedependent p53 acetylation and p21 induction as well as H2AX Phosphorylation.

Cell Cycle Analysis[1]

Cell Line:NCI-H460, A2780, MM473, H460-R9A cells
Concentration:0.25 μM for NCI-H460, 0.6 μM for A2780, 1.2 μM for MM473, 2.8 μM for H460-R9A
Incubation Time:72 h
Result:Cells were arrested at the G1-S phase.
体内研究
(In Vivo)

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%)[1].
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[1].
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)[1].

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)[1]
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)[1]
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).
分子量

461.55

Formula

C28H31NO5

CAS 号

2217671-64-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.