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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
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
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Spezifikationsblatt ansehen →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Klasse | 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 |
| Beschreibung | 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 |
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Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Datum | Artikel |
|---|---|---|---|
 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 |
| Löslichkeit | Solubility (25°C) In vitro DMSO: 96 mg/mL (198.12 mM); Ethanol: 22 mg/mL (45.4 mM); Water: Insoluble; |
|---|---|
| DMSO (mg/ml) Maximale Löslichkeit | 96 |
| DMSO (mM) Maximale Löslichkeit | 198.1260577 |
| Wasser (mg/ml) Maximale Löslichkeit | ＜1 |
| Molekulargewicht | 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 |
