≥99% pour les flux de travail chromatographiques et analytiques sensibles nécessitant une interférence de ligne de base minimale.
Store at -20°C Expédition Ice chest + Ice pads. Consultez le COA spécifique au lot pour les spécifications exactes.
SDS, COA, fiche technique et fiche de spécifications disponibles au téléchargement. COA spécifique au lot accessible via la recherche par numéro de lot.
Cité dans 0 publications à comité de lecture couvrant la chromatographie, la synthèse organique et les réactions de couplage croisé.
Information
MI-463 MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
Targets
Menin-MLL interaction (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.
Cell Research(from reference)
Cell lines：leukemia cells
Incubation Time：6 or 7 days
Document complet couvrant les dangers, la manipulation, le stockage et la conformité réglementaire.
<<<<<<< HEAD Télécharger la SDS → ======= Télécharger la SDS → >>>>>>> release248-p3Données qualité spécifiques au lot. Saisissez votre numéro de lot pour récupérer le COA exact.
Rechercher le COA →Résumé de référence rapide des spécifications et applications du produit.
Voir la fiche technique →Attributs de qualité complets et critères d'acceptation pour cette qualité.
Voir la fiche de spécifications →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Classe | Thienopyrimidines |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Thienopyrimidines |
| Alternative Parents | Indoles 2,3,5-trisubstituted thiophenes Aralkylamines Aminopyrimidines and derivatives Substituted pyrroles Piperidines Imidolactams Benzenoids Heteroaromatic compounds Trialkylamines Nitriles Azacyclic compounds Organofluorides Hydrocarbon derivatives Alkyl fluorides |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Indole - Indole or derivatives - Thienopyrimidine - 2,3,5-trisubstituted thiophene - Aminopyrimidine - Aralkylamine - Piperidine - Pyrimidine - Imidolactam - Benzenoid - Substituted pyrrole - Heteroaromatic compound - Pyrrole - Thiophene - Tertiary aliphatic amine - Tertiary amine - Azacycle - Nitrile - Carbonitrile - Alkyl halide - Alkyl fluoride - Organonitrogen compound - Organofluoride - Organohalogen compound - Hydrocarbon derivative - Cyanide - Organic nitrogen compound - Amine - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as thienopyrimidines. These are heterocyclic compounds containing a thiophene ring fused to a pyrimidine ring. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Article |
|---|---|---|---|
 I2611088 | Certificate of Analysis | Sep 22, 2026 | M413841 |
| C2308215 | Certificate of Analysis | Dec 12, 2025 | M413841 |
| C23071014 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071015 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071021 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071043 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071057 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071064 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| C23071075 | Certificate of Analysis | Nov 21, 2022 | M413841 |
| Solubilité | Solubility (25°C) In vitro DMSO: 96 mg/mL (198.12 mM); Ethanol: 22 mg/mL (45.4 mM); Water: Insoluble; |
|---|---|
| DMSO (mg/mL) Solubilité maximale | 96 |
| DMSO (mM) Solubilité maximale | 198.1260577 |
| Eau (mg/mL) Solubilité maximale | ＜1 |
| Poids moléculaire | 484.500 g/mol |
| XLogP3 | 5.900 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 5 |
| Exact Mass | 484.166 Da |
| Monoisotopic Mass | 484.166 Da |
| Topological Polar Surface Area | 109.000 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 751.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
