STM2457 is a first-in-class, potent and specific, orally active METTL3 inhibitor with an IC50 of 16.9 nM and excellent in vivo activity without off-target effects.
| Cell Experiment | |
|---|---|
| Cell lines | MOLM-13 cells |
| Preparation method | Western blot analysis Cells were treated with Vehicle (DMSO) or the indicated concentrations of STM2457 and after 72 hours cell pellets resuspended in whole cell lysis buffer (50 mM Tris-HCl pH=8, 450 mM NaCl, 0.1% NP-40, 1mM EDTA), supplemented with 1 mM DTT, protease inhibitors, and phosphatase inhibitors. Protein concentrations were assessed by Bradford assay and an equal amount of protein was loaded per track. Prior to loading, the samples were supplemented with SDS-PAGE sample buffer and DTT was added to each sample. 10-40 μg of protein was separated on SDS-PAGE gels, and blotted onto polyvinylidene difluoride membranes. |
| Concentrations | 1, 5 and 10 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | 6- to 10-week-old NSG female mice |
| Formulation | dissolved in 20%(w/v) 2-hydroxyproply beta-cyclodextrin vehicle |
| Dosages | 50 mg/kg |
| Administration | intraperitoneal injection |
| Molecular Weight | 444.53 |
| Formula | C25H28N6O2 |
| CAS Number | 2499663-01-1 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related METTL3 Products |
|---|
| METTL3-IN-4
METTL3-IN-4 is a METTL3 inhibitor. |
| STM2120
STM2120 is a METTL3-METTL14 inhibitor with an IC50 of 64.5 μM. |
| 7OQL
7OQL is a selective METTL3 inhibitor (IC50=0.054 µM). |
| STC-15
STC-15 is a METTL3 inhibitor used in the study of proliferative diseases such as cancer and autoimmune diseases. |
| UZH2
UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM. |
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