2. Epigenetics
  3. Epigenetic Reader Domain
  4. M-1211

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

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

M-1211 Chemical Structure

M-1211 Chemical Structure

CAS No. : 2377337-93-2

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5 mg USD 2350 In-stock
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Based on 1 publication(s) in Google Scholar

M-1211 Related Antibodies

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Description

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]
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.

M-1211 Related Antibodies

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.
Molecular Weight

793.00

Formula

C42H57FN6O6S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2610 mL 6.3052 mL 12.6103 mL
5 mM 0.2522 mL 1.2610 mL 2.5221 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 (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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.29%

COA (254 KB) HNMR (240 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

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 (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.

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
5 mM 0.2522 mL 1.2610 mL 2.5221 mL 6.3052 mL
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M-1211 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-12112377337-93-2M1211M 1211Epigenetic Reader DomaincovalentinteractionscysteineMLLmeninpotentlytranslocationsInhibitorinhibitorinhibit

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