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M-1211 

Cat. No.: HY-132234
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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.

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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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].

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].

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.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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M-1211
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HY-132234
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