MI-463 (C005B-308893)

Biochem/physiol Actions

MI-463 is an orally active and potent menin-MLL interaction inhibitor (cell-free IC50 = 15.3 nM against 1 nM FITC-MLL(4-13) peptide) that targets menin MLL-binding site with high affinity (KD = 9.9 nM by ITC). MI-463 selectively inhibits mixed lineage leukemia (MLL) oncogenic fusion-driven cancer progression in cultures (GI50 by MTT = 230 nM vs. >5 μM against murine BMCs with or without MLL-AF9 fusion transformation) and is efficacious against human MLL leukemia MV4;11 tumor growth in mice in vivo (35 mg/kg/day i.p.) and improve the survival of MLL leukemic mice (40-50 mg/kg b.i.d. p.o.).

UPC:

12161502

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

25

Unit of Measurement:

MG

MPN:

SML3496-25MG

CAS:

1628317-18-9