| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C42H57FN6O6S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
M-1211 is a covalent, orally active inhibitor of the menin-MLL interaction capable of achieving complete, persistent tumor regression[1]. It is supplied as a white to yellow solid (C42H57FN6O6S, MW 793.00) at 99.29% purity.
Physical & Chemical Properties
| CAS Number | 2377337-93-2 |
|---|---|
| Molecular Formula | C42H57FN6O6S |
| Molecular Weight | 793.00 g/mol |
| Purity | 99.29% |
| 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 |
| Signaling Pathway | Epigenetics |
| Solubility | In Vitro: DMSO: 7.69 mg/mL (9.70 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| 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). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 7.69 mg/mL (9.70 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In the MLL-rearranged MV4;11 leukemia cell line, M-1121 (0~100 nM; 24 hours; MV4;11 cells) down-regulates HOXA9 and MEIS1 gene expression in a dose-dependent manner[1]. M-1121 forms covalent interactions with Cysteine 329 within the pocket of menin that binds MLL, and potently inhibits the growth of acute leukemia cell lines with MLL translocations but is inactive in cell lines with wild-type MLL[1].
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) lowers the average tumor volume from 157 mm3 at treatment start to 106 mm3 on day 26, a 32% reduction in tumor volume[1]. M-1121 (300 mg/kg; p.o.) results in complete tumor regression in 10 out of 10 mice, with no tumor regrowth detected for up to a month after the last treatment[1]. M-1121 (5 mg/kg; p.o.) shows low clearance and a moderate volume of distribution[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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