[CAS NO. 1857417-13-0] MI-503
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PRODUCTS SPECIFICATIONS [1857417-13-0]
Catalog
SLK-S7817
Brand
Selleck
CAS
1857417-13-0
DESCRIPTION [1857417-13-0]
Overview
| MDL | MFCD28506303 |
|---|---|
| Molecular Weight | 564.63 |
| Molecular Formula | C28H27F3N8S |
| SMILES | N#CC(N1CC2=CNN=C2)=CC3=C1C=CC(CN4CCC(NC5=C(C=C(CC(F)(F)F)S6)C6=NC=N5)CC4)=C3C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7711 mL | 8.8554 mL | 17.7107 mL |
| 5 mM | 0.3542 mL | 1.7711 mL | 3.5421 mL |
| 10 mM | 0.1771 mL | 0.8855 mL | 1.7711 mL |
| 50 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL |
Description
MI-503 is a potent and selective inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.
Targets
| Menin-MLL interaction [1] (Cell-free assay) |
| 14.7 nM |
In vitro
Treatment of murine bone marrow cells (BMC) transformed with the MLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with half-maximal growth inhibitory concentration (GI50) values of 0.22 μM, measured after 7 days of treatment. The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced effect achieved after 7-10 days of treatment. MI-503 is also very effective in inducing differentiation of MLL leukemia cells and substantially increases expression of CD11b, a myeloid differentiation marker. These effects are accompanied by reduced c-kit (CD117) expression, a marker associated with leukemia stem cells (LSCs). Treatment with sub-micromolar concentrations of MI-503 also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias.
In vivo
MI-503 has very favorable drug-like properties, including metabolic stability and pharmacokinetic profile in mice. It blocks hematologic tumors in vivo and reduces MLL leukemia tumor burden. MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (~75%). Prolonged treatment (38 days) with MI-503 induces no toxicity in mice as reflected by no alterations in the body weight and no morphological changes in liver and kidney tissues. MI-503 could substantially improve survival of MLL leukemic mice and does not impair normal hematopoiesis in vivo.
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