MI-538

Name: MI-538
Brand: MedChemExpress
SKU: HY-19810
Rating: 5.0 (4 reviews)

製品番号: HY-19810 純度: 98.23%: Data Sheet SDS COA 取扱説明書
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MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC₅₀ of 21 nM.

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MI-538 構造式

CAS 番号 : 1857417-10-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 299	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 299	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$132	在庫あり	Estimated Time of Arrival: December 31
5 mg	$240	在庫あり	Estimated Time of Arrival: December 31
10 mg	$420	在庫あり	Estimated Time of Arrival: December 31
25 mg	$756	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1134	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1580	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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This product is a controlled substance and not for sale in your territory.

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Based on 4 publication(s) in Google Scholar

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製品説明

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]

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]
HL-60	GI₅₀	>6 μM 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	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]
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]
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]

体外実験

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.

体内実験

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.

分子量

566.60

分子式

C₂₇H₂₅F₃N₈OS

CAS 番号

1857417-10-7

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.23%

Select Batch:

データシート (275 KB) SDS (393 KB)

COA (248 KB) HNMR (153 KB) RP-HPLC (225 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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]

Complete Stock Solution Preparation Table

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

MI-538 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MI-5381857417-10-7MI538MI 538Epigenetic Reader DomainInhibitorinhibitorinhibit

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MI-538

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MI-538 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

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参考文献

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MI-538 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MI-538 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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