Determine the necessary mass, volume, or concentration for preparing a solution.
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Moligand™, 10mM in DMSO Moligand™ para flujos de trabajo cromatográficos y analíticos sensibles que requieren una interferencia mínima de la línea base.
Store at -80°C Envío Dry ice packs + Cold packs. Consulte el COA específico del lote para conocer las especificaciones exactas.
SDS, COA, ficha técnica y hoja de especificaciones disponibles para descargar. COA específico del lote accesible mediante búsqueda por número de lote.
Citado en 0 publicaciones revisadas por pares sobre cromatografía, síntesis orgánica y reacciones de acoplamiento cruzado.
Product Describtion:
BMS-911543 is a selective small-molecule inhibitor of JAK2 with IC50 value of 1.1nM .
BMS-911543 is a reversible pyrrolopyridine ATP-competitive JAK2 inhibitor with a high selectivity. In the in vitro assay using human recombinant JAK enzyme, BMS-911543 displays an IC50 value of 1.1nM against JAK2 and the Ki value is 0.48nM. The inhibition activity and affinity against JAK2 are both much higher than those against JAK1 and JAK3. Besides that, BMS-911543 also has efficacy against other kinases, such as Lyn and the c-FMS receptor tyrosine kinase. In JAK-dependent cells such as SET2 or Ba/F3, the treatment of BMS-911543 causes an anti-proliferative effect with IC50 values of 60 and 70nM, respectively. The cell lines depending on other JAK family members do not show significant anti-proliferative response to BMS-911543. The colony growth assays prove that BMS-911543 can suppress the growth of MPN patient-derived cells and is more potent in the JAK2V617F pathway compared with the JAK2WT pathway. BMS-911543 is also found to be potent in vivo in both the JAK2WT pathway and the JAK2V617F pathway through suppressing pSTAT5 induction .
Documento completo sobre peligros, manipulación, almacenamiento y cumplimiento normativo.
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Ver hoja de especificaciones →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Clase | Pyrrolopyridines |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Pyrrolopyridines |
| Alternative Parents | Imidazo-[4,5-c]pyridines Pyrrole carboxamides 2-heteroaryl carboxamides Aminopyridines and derivatives Substituted pyrroles N-substituted imidazoles Imidolactams Tertiary carboxylic acid amides Pyrazoles Heteroaromatic compounds Azacyclic compounds Organooxygen compounds Organic oxides Hydrocarbon derivatives Amines |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Imidazopyridine - Pyrrolopyridine - Imidazo-[4,5-c]pyridine - 2-heteroaryl carboxamide - Pyrrole-2-carboxamide - Pyrrole-2-carboxylic acid or derivatives - Aminopyridine - Imidolactam - Substituted pyrrole - Pyridine - N-substituted imidazole - Heteroaromatic compound - Azole - Tertiary carboxylic acid amide - Pyrrole - Imidazole - Pyrazole - Carboxamide group - Azacycle - Carboxylic acid derivative - Amine - Hydrocarbon derivative - Organic nitrogen compound - Organic oxygen compound - Organic oxide - Organooxygen compound - Organonitrogen compound - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as pyrrolopyridines. These are compounds containing a pyrrolopyridine moiety, which consists of a pyrrole ring fused to a pyridine. Pyrrole is 5-membered ring consisting of four carbon atoms and one nitrogen atom. Pyridine is a 6-membered ring consisting of five carbon atoms and one nitrogen center. |
| External Descriptors | Not available |
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| Peso molecular | 432.500 g/mol |
|---|---|
| XLogP3 | 2.900 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 6 |
| Exact Mass | 432.239 Da |
| Monoisotopic Mass | 432.239 Da |
| Topological Polar Surface Area | 85.800 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 717.000 |
| 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 |
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