Size | Price | Stock | Qty |
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1mg |
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Other Sizes |
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Targets |
menin-MLL interaction[1]
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ln Vitro |
In the MLL-rearranged MV4;11 leukemia cell line, M-1121 (0~100 nM; 24 hours; MV4;11 cells) induces dose-dependent down-regulation of HOXA9 and MEIS1 gene expression[1]. M-1121 forms covalent bonds with Cysteine 329, which is found in the menin MLL binding pocket. This effectively suppresses the proliferation of acute leukemia cell lines that have MLL translocations, while having no effect on cell lines that have wild-type MLL[1].
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ln Vivo |
M-1121 (100 mg/kg; po; 26 days) results in a 32% reduction in tumor volume, with the average tumor volume decreasing from 157 mm3 at treatment initiation to 106 mm3 on day 26[1]. In 10 of the 10 mice treated with M-1121 (300 mg/kg; po), all tumors completely recede, and no tumor growth is seen for up to one month following the last treatment[1]. M-1121 has a modest volume of distribution and a low clearance at 5 mg/kg; po[1].
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Cell Assay |
RT-PCR[1]
Cell Types: MV4;11 cells Tested Concentrations: 0~100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Drived dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line. |
Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse[1]
Doses: 100 mg/kg Route of Administration: Po Experimental Results: diminished 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/Disease Models: SCID (severe combined immunodeficient) mouse[1] Doses: 300 mg/kg Route of Administration: Po Experimental Results: Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment. Animal/Disease Models: Female C57BL/6 mice[1] Doses: 5 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Po Experimental Results: Had a low clearance and a moderate volume of distribution. |
References |
[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.
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Molecular Formula |
C42H57FN6O6S
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Molecular Weight |
793.00
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CAS # |
2377337-93-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[C@](C1C=CC=C(F)C=1)(C1CCN(CC2(CN(C3C=CC(S(N4C[C@H]5N(C(=O)C=C)C[C@@H]4C5)(=O)=O)=CC=3)C2)OC)CC1)([C@@]1([H])CCC[C@@H]1NC(=O)OC)CN1CCC1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.