Art. -Nr.: HY-19810

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MI-538

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC₅₀ of 21 nM.

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Reinheit: 98.23%
CAS. Nr.: 1857417-10-7
Formel: C₂₇H₂₅F₃N₈OS
Molecular Weight:566.60

Speicherung:

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

MI-538 Chemical Structure

CAS. Nr.: 1857417-10-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC₅₀ of 21 nM.

IC₅₀ & Target

IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	GI₅₀	0.083 μM Compound: 27; MI-538	Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay	[PMID: 26744767]
Bone marrow cell	GI₅₀	9 μM Compound: 27; MI-538	Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay	[PMID: 26744767]
HL-60	GI₅₀	>6000 nM Compound: 27; MI-538	Growth inhibition of human HL60 after 7 days by MTT assay Growth inhibition of human HL60 after 7 days by MTT assay	[PMID: 26744767]
K562	EC₅₀	2.7 μM Compound: MI-538	Cytotoxicity against human K562 cells measured after 48 hrs by MTT assay Cytotoxicity against human K562 cells measured after 48 hrs by MTT assay	[PMID: 35569690]
MOLM-13	GI₅₀	268 nM Compound: 27; MI-538	Growth inhibition of human MOLM13 after 7 days by MTT assay Growth inhibition of human MOLM13 after 7 days by MTT assay	[PMID: 26744767]
MOLM-13	EC₅₀	0.14 μM Compound: MI-538	Cytotoxicity against human MOLM-13 cells measured after 48 hrs by MTT assay Cytotoxicity against human MOLM-13 cells measured after 48 hrs by MTT assay	[PMID: 35569690]
MV4-11	GI₅₀	175 nM Compound: 27; MI-538	Growth inhibition of human MV4-11 after 7 days by MTT assay Growth inhibition of human MV4-11 after 7 days by MTT assay	[PMID: 26744767]

In Vitro

MI-538 inhibits the proliferation of MLL leukemia cells with a GI₅₀ of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (K_d=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression^[1].

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

In Vivo

Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)^[1].

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

Chemical Information

CAS. Nr. 1857417-10-7
Appearance Solid
Molecular Weight 566.60
Formel C₂₇H₂₅F₃N₈OS
Color White to off-white
SMILES

FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=C(O)C=C(N(CC5=CNN=C5)C(C#N)=C6)C6=C4)CC3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (4)

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Journal Impact Factor

Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Cells

Unlike Its Paralog LEDGF/p75, HRP-2 Is Dispensable for MLL-R Leukemogenesis but Important for Leukemic Cell Survival. [Abstract]

2021 Jan 19;10(1):192. PMID: 33477970
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835
Res Sq

2026 Jan 20.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (176.49 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

1.7649 mL

8.8246 mL

17.6491 mL

5 mM

0.3530 mL

1.7649 mL

3.5298 mL

10 mM

0.1765 mL

0.8825 mL

1.7649 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.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 10 mg/mL (17.65 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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% Corn Oil

Solubility: ≥ 10 mg/mL (17.65 mM); Clear solution

This protocol yields a clear solution of ≥ 10 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 (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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

Solubility: 2.08 mg/mL (3.67 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Protokoll

Cell Assay^[1]

MOLM-13, MV4;11, HL-60 human leukemia cells as well as MLL-AF9 and HM-2 murine bone marrow cells are treated with MI-538 or 0.25% DMSO for 7 days. Media are changed at day 4 with viable cell number restored to the original concentration, and MI-538 are resupplied. An amount of 100 μL of cell suspension is transferred to 96-well plates for each sample in quadruplicates. Cell viability is measured using the MTT assay. Plates are read for absorbance at 570 nm^[1].

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

Animal Administration^[1]

Mice: Mice xenograft are randomly grouped with each group containing eight mice. Vehicle or MI-538 (45 mg/kg) are administrated once daily at designated doses using ip injections for 2 weeks. Body weight and tumor sizes are monitored three times a week^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Borkin D, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913. [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	1.7649 mL	8.8246 mL	17.6491 mL	44.1228 mL
	5 mM	0.3530 mL	1.7649 mL	3.5298 mL	8.8246 mL
	10 mM	0.1765 mL	0.8825 mL	1.7649 mL	4.4123 mL
	15 mM	0.1177 mL	0.5883 mL	1.1766 mL	2.9415 mL
	20 mM	0.0882 mL	0.4412 mL	0.8825 mL	2.2061 mL
	25 mM	0.0706 mL	0.3530 mL	0.7060 mL	1.7649 mL
	30 mM	0.0588 mL	0.2942 mL	0.5883 mL	1.4708 mL
	40 mM	0.0441 mL	0.2206 mL	0.4412 mL	1.1031 mL
	50 mM	0.0353 mL	0.1765 mL	0.3530 mL	0.8825 mL
	60 mM	0.0294 mL	0.1471 mL	0.2942 mL	0.7354 mL
	80 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5515 mL
	100 mM	0.0176 mL	0.0882 mL	0.1765 mL	0.4412 mL

Keywords

MI-538

4 Cited Publications

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MI-538

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MI-538

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MI-538

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MI-538

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MI-538 Related Classifications

HY-19810 Related Classifications