Art. -Nr.: HY-143412

MIR002

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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.

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Reinheit: 99.0%
CAS. Nr.: 2217671-64-0
Formel: C₂₇H₂₉NO₅
Molecular Weight:447.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

MIR002 Chemical Structure

CAS. Nr.: 2217671-64-0

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Preis

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HDAC11

6.09 μM (IC₅₀)

DNA Polymerase

POLA1

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

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].

MedChemExpress (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].

MedChemExpress (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).

Chemical Information

CAS. Nr. 2217671-64-0
Appearance Solid
Molecular Weight 447.52
Formel C₂₇H₂₉NO₅
Color White to off-white
SMILES

ONC(COC1=C(C=C(C2=CC=C(C=C2)/C=C/C(O)=O)C=C1)C34CC5CC(CC(C5)C4)C3)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (223.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2345 mL

11.1727 mL

22.3454 mL

5 mM

0.4469 mL

2.2345 mL

4.4691 mL

10 mM

0.2235 mL

1.1173 mL

2.2345 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022, 228:113971. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2345 mL	11.1727 mL	22.3454 mL	55.8634 mL
	5 mM	0.4469 mL	2.2345 mL	4.4691 mL	11.1727 mL
	10 mM	0.2235 mL	1.1173 mL	2.2345 mL	5.5863 mL
	15 mM	0.1490 mL	0.7448 mL	1.4897 mL	3.7242 mL
	20 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	25 mM	0.0894 mL	0.4469 mL	0.8938 mL	2.2345 mL
	30 mM	0.0745 mL	0.3724 mL	0.7448 mL	1.8621 mL
	40 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	50 mM	0.0447 mL	0.2235 mL	0.4469 mL	1.1173 mL
	60 mM	0.0372 mL	0.1862 mL	0.3724 mL	0.9311 mL
	80 mM	0.0279 mL	0.1397 mL	0.2793 mL	0.6983 mL
	100 mM	0.0223 mL	0.1117 mL	0.2235 mL	0.5586 mL

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MIR002

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MIR002

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MIR002 Related Classifications

HY-143412 Related Classifications