[CAS NO. 1857417-10-7] MI-538
PRODUCTS SPECIFICATIONS [1857417-10-7]
DESCRIPTION [1857417-10-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 566.60 |
| Molecular Formula | C27H25F3N8OS |
| SMILES | FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=C(O)C=C(N(CC5=CNN=C5)C(C#N)=C6)C6=C4)CC3 |
2 Publications Citing Use of MCE
Summary
MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC 50 of 21 nM.
IC50 & Target
IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin) [1]
In Vitro
MI-538 inhibits the proliferation of MLL leukemia cells with a GI 50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (K d =6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 176.49 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7649 mL | 8.8246 mL | 17.6491 mL |
| 5 mM | 0.3530 mL | 1.7649 mL | 3.5298 mL |
| 10 mM | 0.1765 mL | 0.8825 mL | 1.7649 mL |