1. Epigenetics
    Cell Cycle/DNA Damage
    Apoptosis
  2. HDAC
    DNA/RNA Synthesis
    Apoptosis
  3. MIR002

MIR002 

Cat. No.: HY-143412
Handling Instructions

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.

For research use only. We do not sell to patients.

MIR002 Chemical Structure

MIR002 Chemical Structure

CAS No. : 2217671-64-0

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Description

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[1].

IC50 & Target

HDAC11

6.09 μM (IC50)

POLA1

 

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 IC50 of 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Molecular Weight

461.55

Formula

C28H31NO5

CAS No.
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MIR002
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