SML3496

MI-463

≥98% (HPLC)

• Synonyme(s) : 4-Methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indole-2-carbonitrile, MI 463, MI463
• Formule empirique (notation de Hill): C₂₄H₂₃F₃N₆S
• Numéro CAS: 1628317-18-9
• Poids moléculaire : 484.54
• Numéro MDL: MFCD28506301
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: -10 to -25°C
• Chaîne SMILES: N#CC1=CC2=C(C)C(CN3CCC(CC3)NC4=C5C=C(CC(F)(F)F)SC5=NC=N4)=CC=C2N1
• Clé InChI: DZACSLYTXLZAAF-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

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.).

Orally active and potent menin-MLL interaction inhibitor that selectively inhibits MLL oncogenic fusions-driven cancer progression in vitro and in vivo.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable