[CAS NO. 2029049-79-2] ML390
PRODUCTS SPECIFICATIONS [2029049-79-2]
DESCRIPTION [2029049-79-2]
Overview
| MDL | MFCD30489750 |
|---|---|
| Molecular Weight | 406.40 |
| Molecular Formula | C21H21F3N2O3 |
| SMILES | O=C(NCCC(N[C@H]1C(C=CC=C2)=C2CCC1)=O)C3=CC=C(OC(F)(F)F)C=C3 |
Summary
ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models [1] [2] [3] .
In Vitro
ML390 is active with an ED
50
of ~2 μM in murine and human AML cell lines. In vitro, treatment of Lys-GFP-ER-HoxA9 cells with ML390 for 48 hr inhibits DHODH activity, leading to the dramatic (>500-fold) accumulation of the upstream metabolite DHO and the depletion of uridine and other downstream metabolites
[2]
.
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 : ≥ 27 mg/mL ( 66.44 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4606 mL | 12.3032 mL | 24.6063 mL |
| 5 mM | 0.4921 mL | 2.4606 mL | 4.9213 mL |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4606 mL |
References
- [1] Sykes DB et al. Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia. National Center for Biotechnology Information (US); 2010-2013 Dec 15.
- [2] David B Sykes, et al. Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia. Cell. 2016 Sep 22;167(1):171-186.e15.
- [3] Timothy A Lewis, et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett. 2016 Sep 28;7(12):1112-1117.