ChemicalBook > CAS DataBase List > 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride

8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride

Product Name
8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride
CAS No.
1942919-79-0
Chemical Name
8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride
Synonyms
NVP-BSK805 2HCl ，S2686;NVP-BSK805 2HCl (BSK-805);8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride
CBNumber
CB94657955
Molecular Formula
C27H29ClF2N6O
Formula Weight
527.02
MOL File
1942919-79-0.mol
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8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Property

storage temp. 
Store at -20°C
solubility 
DMF: 20 mg/ml; DMSO: 25 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 10 mg/ml
form 
A crystalline solid
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16714
Product name
NVP-BSK805 (hydrochloride)
Packaging
1mg
Price
$68
Updated
2024/03/01
Cayman Chemical
Product number
16714
Product name
NVP-BSK805 (hydrochloride)
Packaging
10mg
Price
$401
Updated
2024/03/01
Cayman Chemical
Product number
16714
Product name
NVP-BSK805 (hydrochloride)
Packaging
5mg
Price
$286
Updated
2024/03/01
ChemScene
Product number
CS-2287
Product name
NVP-BSK805(dihydrochloride)
Purity
99.36%
Packaging
5mg
Price
$168
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD146326
Product name
NVP BSK 805 dihydrochloride
Packaging
10mg
Price
$185
Updated
2021/12/16
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8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Chemical Properties,Usage,Production

Description

Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family. A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer. NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases. This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice. NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats. NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells.

Uses

NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].

in vivo

NVP-BSK805 (BSK805 dihydrochloride; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].

IC 50

JAK2 JH1: 0.48 nM (IC50); FL JAK2 V617F: 0.56 nM (IC50); FL JAK2 wt: 0.58 nM (IC50); TYK2 JH1: 10.76 nM (IC50); JAK3 JH1: 18.68 nM (IC50); JAK1 JH1: 31.63 nM (IC50)

References

[1] Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55. DOI:10.1158/1535-7163.MCT-10-0053
[2] Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182. DOI:10.1016/j.bbrc.2017.06.178

8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Suppliers

China 18 United States 4 Global 22
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
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China
ProdList
4768
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Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
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60
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9125
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Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
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58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
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58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
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11218
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58
InvivoChem
Tel
13549236410
Email
sales@invivochem.cn
Country
China
ProdList
6753
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58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
Tel
021-59167510 18117107507
Email
vip@med-life.cn
Country
China
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5002
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Shanghai Aladdin Biochemical Technology Co.,Ltd.
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400-6206333 13167063860
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anhua.mao@aladdin-e.com
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China
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48457
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1942919-79-0, 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochlorideRelated Search:

NVP-CGM097 CEP-28122 monomesilate hydrochloride salt CEP-28122 NVP-BSK805

  • 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride
  • NVP-BSK805 2HCl (BSK-805)
  • NVP-BSK805 2HCl ，S2686
  • 1942919-79-0