Cat. No.: HY-125858

MI-1061

Name: MI-1061
Brand: MedChemExpress
SKU: HY-125858
Price: 140.00 USD
Availability: InStock
Rating: 5 (3 reviews)

3 Cited Publications

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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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Top Publications Citing

Use of MCE Products

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
Protocols (10)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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. Further protocols information, click here.

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)

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Dilution Calculator

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

Protocols

All Cell Biology Animals and Diseases Signal Pathway Related

Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 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)
- Korean - KR (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

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MI-1061

Publications Citing Use of MedChemExpress (MCE) MI-1061