Accéder au contenu
Merck
Toutes les photos(1)

Principaux documents

Voir toute la documentation

SML2628

Sigma-Aldrich

NVP-BSK805 Trihydrochloride

≥98% (HPLC)

Synonyme(s) :

4-(2,6-Difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine trihydrochloride, 8-(3,5-Difluoro-4-morpholin-4-ylmethyl-phenyl)-2-(1-piperidin-4-yl-1H-pyrazol-4-yl)-quinoxaline trihydrochloride, 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline trihydrochloride, BSK 805 3HCl, BSK805, 3HCl, NVP-BSK 805 3HCl

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme

Sélectionner une taille de conditionnement

5 MG
62,60 €
25 MG
255,00 €

62,60 €

Veuillez contacter notre Service Clients pour connaître la disponibilité de ce produit.
Devis pour commande en gros
Toutes les photos(1)

Sélectionner une taille de conditionnement

Changer de vue
5 MG
62,60 €
25 MG
255,00 €

About This Item

Formule empirique (notation de Hill):
C27H28F2N6O·3HCl
Numéro CAS:
2320258-95-3
Poids moléculaire :
599.93
Numéro MDL:
MFCD22419018
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

62,60 €

Veuillez contacter notre Service Clients pour connaître la disponibilité de ce produit.
Devis pour commande en gros

Essai

≥98% (HPLC)

Forme

powder

Couleur

faint yellow to dark orange

Solubilité

H2O: 2 mg/mL, clear

Température de stockage

−20°C

Chaîne SMILES 

Fc1c(c(cc(c1)c3c4nc(cnc4ccc3)c5c[n](nc5)C6CCNCC6)F)CN2CCOCC2

InChI

1S/C27H28F2N6O/c28-23-12-18(13-24(29)22(23)17-34-8-10-36-11-9-34)21-2-1-3-25-27(21)33-26(15-31-25)19-14-32-35(16-19)20-4-6-30-7-5-20/h1-3,12-16,20,30H,4-11,17H2

Clé InChI

IBPVXAOOVUAOKJ-UHFFFAOYSA-N

Actions biochimiques/physiologiques

NVP-BSK805 is a selective, ATP-competitive (Ki = 0.43 nM) Janus kinase 2 (JAK2) inhibitor (IC50 = 0.58 and 0.56 nM against full-length wild-type and V617F JAK2, respectively) with greatly reduced potency against TYK2, JAK3, JAK1 (IC50 = 10.76, 18.68, 31.63 nM against respective JAK homology domain 1) and >300-fold selectivity over a panel of 36 other kinases. BSK805 potently inhibits STAT5 phosphorylation (by >90% at 100 nM; MB-02 & SET-2 cells) and proliferation in JAK2V617F mutant cultures in vitro (GI50= 39-331 nM; 75% SET-2 growth inhibition at 150 nM) and in Ba/F3 JAK2V617F-bearing mice in vivo (150 mg/kg p.o.). BSK805 daily oral administration is also efficacious against rhEpo-induced splenomegaly and polycythemia in mice (50-100 mg/kg) and rats (25-50 mg/kg) with good pharmacokinetics and oral avilability.
Orally available, ATP-competitive Janus kinase 2 (JAK2) inhibitor with efficacy against JAK2V617F-driven leukemic disease in mice and rats in vivo.

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

Faites votre choix parmi les versions les plus récentes :

Certificats d'analyse (COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.

Si vous avez besoin d'assistance, veuillez contacter Service Clients

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Alessia Bottos et al.
Nature communications, 7, 12258-12258 (2016-07-14)
The JAK/STAT pathway is an attractive target for breast cancer therapy due to its frequent activation, and clinical trials evaluating JAK inhibitors (JAKi) in advanced breast cancer are ongoing. Using patient biopsies and preclinical models of breast cancer, we demonstrate
M Thorn et al.
Cancer gene therapy, 23(6), 188-198 (2016-05-21)
Assumptions that liver immune cells and immunosuppressive pathways are similar to their counterparts in other spaces have led to gaps in our understanding of intrahepatic neoplasm aggressiveness. Myeloid-derived suppressor cells (MDSCs) are potent inhibitors of antitumor immunity and pose a
Andriy Marusyk et al.
Cancer research, 76(22), 6495-6506 (2016-11-05)
Using a three-dimensional coculture model, we identified significant subtype-specific changes in gene expression, metabolic, and therapeutic sensitivity profiles of breast cancer cells in contact with cancer-associated fibroblasts (CAF). CAF-induced gene expression signatures predicted clinical outcome and immune-related differences in the
Fabienne Baffert et al.
Molecular cancer therapeutics, 9(7), 1945-1955 (2010-07-01)
The recent discovery of an acquired activating point mutation in JAK2, substituting valine at amino acid position 617 for phenylalanine, has greatly improved our understanding of the molecular mechanism underlying chronic myeloproliferative neoplasms. Strikingly, the JAK2(V617F) mutation is found in
Justin M Balko et al.
Science translational medicine, 8(334), 334ra53-334ra53 (2016-04-15)
Amplifications at 9p24 have been identified in breast cancer and other malignancies, but the genes within this locus causally associated with oncogenicity or tumor progression remain unclear. Targeted next-generation sequencing of postchemotherapy triple-negative breast cancers (TNBCs) identified a group of
Afficher tous les articles scientifiques apparentés

Questions

Reviews

No rating value

Active Filters

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique