M-808

Name: M-808
Brand: MedChemExpress
SKU: HY-133738
Rating: 4.5 (0 reviews)

Cat. No.: HY-133738 Purity: 98.72%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC₅₀ value of 2.6 nM.

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

M-808 Chemical Structure

CAS No. : 2377335-74-3

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 1 Customer Validation

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC₅₀ value of 2.6 nM^[1].

IC₅₀ & Target

IC50: 1 nM (Menin-MLL in MV4;11 cells), 4 nM (Menin-MLL in MOLM-13 cells)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	2.8 μM Compound: 16; M-808	Growth inhibition of human HL60 cells after 7 days by WST-8 assay Growth inhibition of human HL60 cells after 7 days by WST-8 assay	[PMID: 32338903]
MOLM-13	IC₅₀	0.004 μM Compound: 16; M-808	Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay	[PMID: 32338903]
MV4-11	IC₅₀	0.001 μM Compound: 16; M-808	Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay	[PMID: 32338903]

In Vitro

M808 exhibits IC₅₀ values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively^[1].
M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin^[1].

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

In Vivo

M-808 (16) is well tolerated in severe combined immunodeficiency (SCID) mice with intravenous administration of 10 mg/kg (or 25 mg/kg) every other day dosing (three times a week) for one week. M-808 (25 mg/kg) achieves a maximum tumor growth inhibition (TGI) of 97% during treatment (day 35) and reduces the average tumor volume from 92 mm³ at the beginning of the treatment to 59 mm³ at day 35, with no significant toxicity^[1].

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

Molecular Weight

819.08

Formula

C₄₅H₆₃FN₆O₅S

CAS No.

2377335-74-3

Appearance

Solid

Color

White to off-white

SMILES

O=S(C(C=C1)=CC=C1N(C2)CC2CN(CC3)CCC3[C@@]([C@@]4([H])CCC[C@@H]4NC(OC)=O)(CN5CCC5)C6=CC(F)=CC=C6)(C7CN(C(/C=C/CN8CCCCC8)=O)C7)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (122.09 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	1.2209 mL	6.1044 mL	12.2088 mL
5 mM	0.2442 mL	1.2209 mL	2.4418 mL
10 mM	0.1221 mL	0.6104 mL	1.2209 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.5 mg/mL (3.05 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 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.05 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.
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.05 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

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

Purity & Documentation

Purity: 98.72%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (247 KB) HNMR (146 KB) RP-HPLC (162 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Shilin Xu, et al. Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction With Strong In Vivo Antitumor Activity. J Med Chem. 2020 May 14;63(9):4997-5010. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2209 mL	6.1044 mL	12.2088 mL	30.5220 mL
	5 mM	0.2442 mL	1.2209 mL	2.4418 mL	6.1044 mL
	10 mM	0.1221 mL	0.6104 mL	1.2209 mL	3.0522 mL
	15 mM	0.0814 mL	0.4070 mL	0.8139 mL	2.0348 mL
	20 mM	0.0610 mL	0.3052 mL	0.6104 mL	1.5261 mL
	25 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2209 mL
	30 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0174 mL
	40 mM	0.0305 mL	0.1526 mL	0.3052 mL	0.7631 mL
	50 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6104 mL
	60 mM	0.0203 mL	0.1017 mL	0.2035 mL	0.5087 mL
	80 mM	0.0153 mL	0.0763 mL	0.1526 mL	0.3815 mL
	100 mM	0.0122 mL	0.0610 mL	0.1221 mL	0.3052 mL

M-808 Related Classifications

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:

M-8082377335-74-3M808M 808Epigenetic Reader DomainMLLleukemialowtoxicityInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

M-808

Customer Review

M-808 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

M-808 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

M-808 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report