Art. -Nr.: HY-132234

M-1211

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M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

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Reinheit: 99.29%
CAS. Nr.: 2377337-93-2
Formel: C₄₂H₅₇FN₆O₆S
Molecular Weight:793.00

Speicherung:

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

M-1211 Chemical Structure

CAS. Nr.: 2377337-93-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression^[1].

IC₅₀ & Target

menin-MLL interaction^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	>10000 nM Compound: 24; M-1121	Anti-proliferative activity against human HL-60 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human HL-60 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
K562	IC₅₀	>10000 nM Compound: 24; M-1121	Anti-proliferative activity against human K562 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human K562 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
KOPN-8	IC₅₀	110 nM Compound: 24; M-1121	Anti-proliferative activity against human KOPN-8 cells harboring MLL/ENL fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human KOPN-8 cells harboring MLL/ENL fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
MEG-01	IC₅₀	>10000 nM Compound: 24; M-1121	Anti-proliferative activity against human MEG-01 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human MEG-01 cells harboring MLL wild-type protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
MOLM-13	IC₅₀	51.5 nM Compound: 24; M-1121	Anti-proliferative activity against human MOLM-13 cells harboring MLL/AF9 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human MOLM-13 cells harboring MLL/AF9 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
MV4-11	IC₅₀	10.3 nM Compound: 24; M-1121	Anti-proliferative activity against human MV4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human MV4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
RS4-11	IC₅₀	1 μM Compound: 24; M-1121	Anti-proliferative activity against human RS4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human RS4-11 cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]
SEM	IC₅₀	51 nM Compound: 24; M-1121	Anti-proliferative activity against human SEM cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay Anti-proliferative activity against human SEM cells harboring MLL/AF4 fusion protein assessed as cell growth inhibition measured after 4 days by Cell Titre Glo Luminescent Cell viability assay	[PMID: 34196551]

In Vitro

M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line^[1].
M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL^[1].

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

RT-PCR^[1]

Cell Line:

MV4;11 cells
Concentration:

0~100 nM
Incubation Time:

24 hours
Result:

Drived dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.

In Vivo

M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm³ at the beginning of the treatment to 106 mm³ on day 26 of the treatment, a reduction of tumor volume of 32%^[1].
M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment^[1].
M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution^[1].

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

Animal Model:

SCID mice^[1]
Dosage:

100 mg/kg
Administration:

P.o.
Result:

Reduced the average tumor volume from 157 mm³ at the beginning of the treatment to 106 mm³ on day 26 of the treatment, a reduction of tumor volume of 32%.

Animal Model:

SCID mice^[1]
Dosage:

300 mg/kg
Administration:

P.o.
Result:

Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.

Animal Model:

Female C57BL/6 mice^[1]
Dosage:

5 mg/kg (Pharmacokinetic Analysis)
Administration:

P.o.
Result:

Had a low clearance and a moderate volume of distribution.

Chemical Information

CAS. Nr. 2377337-93-2
Appearance Solid
Molecular Weight 793.00
Formel C₄₂H₅₇FN₆O₆S
Color White to yellow
SMILES

FC1=CC(C(CN2CCC2)([C@@]3([H])CCC[C@@H]3NC(OC)=O)C4CCN(CC5(OC)CN(C6=CC=C(S(N7C[C@@]8([H])N(C(C=C)=O)C[C@@]7(C8)[H])(=O)=O)C=C6)C5)CC4)=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 7.69 mg/mL (9.70 mM; ultrasonic and warming and heat to 60°C; 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

1.2610 mL

6.3052 mL

12.6103 mL

5 mM

0.2522 mL

1.2610 mL

2.5221 mL

10 mM

---

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)
- 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]. Zhang M, et al. Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression. J Med Chem. 2021;64(14):10333-10349. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2610 mL	6.3052 mL	12.6103 mL	31.5259 mL
DMSO	5 mM	0.2522 mL	1.2610 mL	2.5221 mL	6.3052 mL

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M-1211

MCE Bioactive Compound Library

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