M-1211
Based on 1 Customer Validation
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.29%
- CAS 番号: 2377337-93-2
- 分子式: C42H57FN6O6S
- 分子量:793.00
-
保管条件:
-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)
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
menin-MLL interaction[1]
|
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] |
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.
-
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.
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.
化学情報
-
CAS 番号 2377337-93-2
-
性状 Solid
-
分子量 793.00
-
分子式 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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-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)
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (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)
-
取扱説明書 (2659 KB)
参考文献
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 |
Powered by Bioz