[CAS NO. 1628317-18-9] MI-463
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PRODUCTS SPECIFICATIONS [1628317-18-9]
Catalog
SLK-S7816
Brand
Selleck
CAS
1628317-18-9
DESCRIPTION [1628317-18-9]
Overview
| MDL | MFCD28506301 |
|---|---|
| Molecular Weight | 484.54 |
| Molecular Formula | C24H23F3N6S |
| SMILES | N#CC(N1)=CC2=C1C=CC(CN3CCC(NC4=C(C=C(CC(F)(F)F)S5)C5=NC=N4)CC3)=C2C |
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 | 2.0638 mL | 10.3191 mL | 20.6381 mL |
| 5 mM | 0.4128 mL | 2.0638 mL | 4.1276 mL |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0638 mL |
| 50 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL |
Description
MI-463 is a potent inhibitor of with an IC50 value of 15.3 nM.
Targets
| Menin-MLL interaction [1] (Cell-free assay) |
| 15.3 nM |
In vitro
MI-463 demonstrates profound on-target activity in MLL leukemia cells. MI-463 results in substantial growth inhibition, with half-maximal growth inhibitory concentration (GI50) values of 0.23 μM, measured after 7 days of treatment in MLL leukemia cells. MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias.
In vivo
MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. MI-463 achieves high levels in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability(∼45%). In a mouse xenograft model using MV4;11 human MLL leukemia cells implanted into BALB/c nude mice, MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo.
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