Cat. No.: HY-125858

MI-1061

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC₅₀=4.4 nM; K_i=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.

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

Purity: 99.08%
CAS No.: 1410737-34-6
Formula: C₃₀H₂₆Cl₂FN₃O₄
Molecular Weight:582.45

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MI-1061 Chemical Structure

CAS No.: 1410737-34-6

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(In Japan)

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 4.4 nM (MDM2)^[1]
Ki: 0.16 nM (MDM2)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	>10 μM Compound: 31, MI-1061	Growth inhibition of p53 -/- human HCT116 cells by WST8 assay Growth inhibition of p53 -/- human HCT116 cells by WST8 assay	[PMID: 25496041]
HCT-116	IC₅₀	0.25 μM Compound: 31, MI-1061	Growth inhibition of p53 +/+ human HCT116 cells by WST8 assay Growth inhibition of p53 +/+ human HCT116 cells by WST8 assay	[PMID: 25496041]
KG-1	IC₅₀	>10 μM Compound: MI-1061	Inhibition of cell growth in human KG-1 cells harbouring mutant p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human KG-1 cells harbouring mutant p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
MDA-MB-231	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-231	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-231 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-10-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
MDA-MB-468	IC₅₀	>3 μM Compound: MI-1061	Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay Antiproliferative activity against human MDA-MB-468 cells transfected with CRBN siRNA LQ-021086-11-0002 assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 31560543]
ML-2	IC₅₀	150.7 μM Compound: MI-1061	Inhibition of cell growth in human ML-2 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human ML-2 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
MOLM-13	IC₅₀	76.8 μM Compound: MI-1061	Inhibition of cell growth in human MOLM-13 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human MOLM-13 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
MOLM-14	IC₅₀	143.3 μM Compound: MI-1061	Inhibition of cell growth in human MOLM-14 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human MOLM-14 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
MONO-MAC-6	IC₅₀	>10 μM Compound: MI-1061	Inhibition of cell growth in human MONO-MAC-6 cells harbouring mutant p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human MONO-MAC-6 cells harbouring mutant p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
OCI-AML-5	IC₅₀	374.5 μM Compound: MI-1061	Inhibition of cell growth in human OCI-AML5 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human OCI-AML5 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
RS4-11	IC₅₀	140 nM Compound: MI-1061	Inhibition of cell growth in human RS4-11 cells incubated for 4 days by Lactate dehydrogenase based WST-8 assay Inhibition of cell growth in human RS4-11 cells incubated for 4 days by Lactate dehydrogenase based WST-8 assay	[PMID: 30525597]
SIG-M5	IC₅₀	105.6 μM Compound: MI-1061	Inhibition of cell growth in human SIG-M5 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay Inhibition of cell growth in human SIG-M5 cells harbouring wild-type p53 incubated for 4 days by lactate dehydrogenase-based WST-8 assay	[PMID: 30525597]
SJSA-1	IC₅₀	0.1 μM Compound: 31, MI-1061	Growth inhibition of human SJSA1 cells by WST8 assay Growth inhibition of human SJSA1 cells by WST8 assay	[PMID: 25496041]

In Vitro

MI-1061 achieves IC₅₀=100 and 250 nM in the SJSA-1 and HCT-116 p53^+/+ cell lines, respectively, and has IC₅₀>10000 nM in the p53 knockout cell line HCT-116 p53^–/–cell line^[1].

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

In Vivo

MI-1061 (100 mg/kg; p.o.; daily for 14 days) is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice^[1].

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

Animal Model:

SCID mice bearing SJSA-1 osteosarcoma xenografts^[1]
Dosage:

100 mg/kg
Administration:

P.o.; daily for 14 days
Result:

Demonstrated strong antitumor activity and achieved significant tumor regression.

Chemical Information

CAS No. 1410737-34-6
Appearance Solid
Molecular Weight 582.45
Formula C₃₀H₂₆Cl₂FN₃O₄
Color White to off-white
SMILES

O=C(O)C1=CC=C(NC([C@H](N2)[C@H](C3=CC=CC(Cl)=C3F)[C@]4(C(NC5=C4C=CC(Cl)=C5)=O)C62CCCCC6)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Nat Commun

PROTAC repurposing uncovers a noncanonical binding surface that mediates chemical degradation of nuclear receptors. [Abstract]

2025 Nov 6;16(1):9805. PMID: 41198675
Cell Rep

MDM2 binds and ubiquitinates PARP1 to enhance DNA replication fork progression. [Abstract]

2022 May 31;39(9):110879. PMID: 35649362
Cells

PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]

2026 Mar 5;15(5):473. PMID: 41827906

Solvent & Solubility

In Vitro:

DMSO : 160 mg/mL (274.70 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

1.7169 mL

8.5844 mL

17.1689 mL

5 mM

0.3434 mL

1.7169 mL

3.4338 mL

10 mM

0.1717 mL

0.8584 mL

1.7169 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 4 mg/mL (6.87 mM); Clear solution

This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: 4 mg/mL (6.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 4 mg/mL (6.87 mM); Clear solution

This protocol yields a clear solution of ≥ 4 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 (40.0 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 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)

References

[1]. Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannichring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014 Dec 26;57(24):10486-98. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7169 mL	8.5844 mL	17.1689 mL	42.9221 mL
	5 mM	0.3434 mL	1.7169 mL	3.4338 mL	8.5844 mL
	10 mM	0.1717 mL	0.8584 mL	1.7169 mL	4.2922 mL
	15 mM	0.1145 mL	0.5723 mL	1.1446 mL	2.8615 mL
	20 mM	0.0858 mL	0.4292 mL	0.8584 mL	2.1461 mL
	25 mM	0.0687 mL	0.3434 mL	0.6868 mL	1.7169 mL
	30 mM	0.0572 mL	0.2861 mL	0.5723 mL	1.4307 mL
	40 mM	0.0429 mL	0.2146 mL	0.4292 mL	1.0731 mL
	50 mM	0.0343 mL	0.1717 mL	0.3434 mL	0.8584 mL
	60 mM	0.0286 mL	0.1431 mL	0.2861 mL	0.7154 mL
	80 mM	0.0215 mL	0.1073 mL	0.2146 mL	0.5365 mL
	100 mM	0.0172 mL	0.0858 mL	0.1717 mL	0.4292 mL

Keywords

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MI-1061

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) MI-1061

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

MI-1061 Related Classifications

Cat. No.: HY-125858