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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

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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

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

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Ji Hyun Cheon et al.
Biochemical and biophysical research communications, 490(4), 1176-1182 (2017-07-04)
P-glycoprotein (P-gp) is overexpressed in cancer cells in order to pump out chemotherapeutic drugs, and is one of the major mechanisms responsible for multidrug resistance (MDR). It is important to identify P-gp inhibitors with low toxicity to normal cells in
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
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
Carole Pissot-Soldermann et al.
Bioorganic & medicinal chemistry letters, 20(8), 2609-2613 (2010-03-17)
We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compounds from this series
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
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