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Merck
CN
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安全信息

SML2628

Sigma-Aldrich

NVP-BSK805 Trihydrochloride

≥98% (HPLC)

别名:

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

经验公式（希尔记法）:
C27H28F2N6O·3HCl
CAS号:
2320258-95-3
分子量:
599.93
MDL编号:
MFCD22419018
UNSPSC代码:
12352200
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

faint yellow to dark orange

溶解性

H2O: 2 mg/mL, clear

储存温度

−20°C

SMILES字符串

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

生化/生理作用

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.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000074553
0000074552
0000068416

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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
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
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
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
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