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SML2628

Sigma-Aldrich

NVP-BSK805 Trihydrochloride

≥98% (HPLC)

Sinónimos:

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

Fórmula empírica (notación de Hill):
C27H28F2N6O·3HCl
Número de CAS:
2320258-95-3
Peso molecular:
599.93
MDL number:
MFCD22419018
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

faint yellow to dark orange

solubility

H2O: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

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

InChI key

IBPVXAOOVUAOKJ-UHFFFAOYSA-N

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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