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NS-018 (hydrochloride)

Product Name
NS-018 (hydrochloride)
CAS No.
1239358-85-0
Chemical Name
NS-018 (hydrochloride)
Synonyms
NS-018 (hydrochloride);Ilginatinib hydrochloride;Ilginatinib (NS-018) hydrochloride;Ilginatinibhydrochloride(NS-018 HCI);Ilginatinib hydrochloride, 10 mM in DMSO;ILGINATINIB HYDROCHLORIDE (NS-018 HYDROCHLORIDE);(S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine hydrochloride;Tyk2,Ilginatinib,JAK1,JAK,JAK2,Inhibitor,bioavailable,NS018,NS-018,orally,inhibit,Janus kinase,JAK3,Ilginatinib hydrochloride,NS 018
CBNumber
CB13067014
Molecular Formula
C21H21ClFN7
Formula Weight
425.8897432
MOL File
1239358-85-0.mol
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NS-018 (hydrochloride) Property

storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 35 mg/mL (82.18 mM)
form 
Solid
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5357
Product name
Ilginatinibhydrochloride
Purity
98.02%
Packaging
5mg
Price
$285
Updated
2021/12/16
ChemScene
Product number
CS-5357
Product name
Ilginatinibhydrochloride
Purity
98.02%
Packaging
10mg
Price
$395
Updated
2021/12/16
ChemScene
Product number
CS-5357
Product name
Ilginatinibhydrochloride
Purity
98.02%
Packaging
25mg
Price
$580
Updated
2021/12/16
ChemScene
Product number
CS-5357
Product name
Ilginatinibhydrochloride
Purity
98.02%
Packaging
50mg
Price
$870
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611574
Product name
NS-018 hydrochloride
Packaging
100mg
Price
$912.9
Updated
2021/12/16
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NS-018 (hydrochloride) Chemical Properties,Usage,Production

Description

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

Ilginatinib (NS-018) is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib (NS-018) also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib (NS-018) shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2[1]. Ilginatinib (NS-018) (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). NS-018 (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients[2].

Ilginatinib (NS-018) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model. Ilginatinib (NS-018) (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice[1].

Uses

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

in vivo

Ilginatinib hydrochloride (NS-018 hydrochloride) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model[1].
Ilginatinib hydrochloride (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice[1].

IC 50

JAK2: 0.72 nM (IC50); Tyk2: 22 nM (IC50); JAK1: 33 nM (IC50); JAK3: 39 nM (IC50)

References

[1]. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29. [2]. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

NS-018 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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NS-018 (hydrochloride) Suppliers

China 27 United States 5 Global 32
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2988
Advantage
58
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel
86-571-88216897,88216896 13588875226
Fax
86-571-88216895
Email
sales@hzclap.com
Country
CHINA
ProdList
6312
Advantage
58
Absin Bioscience Inc.
Tel
021-38015121 18438616290
Email
lanwu@univ-bio.com
Country
China
ProdList
24731
Advantage
58
Shanghai Luofa Biochemical Technology Co., Ltd.
Tel
021-51111890 15317326293
Email
sales@molnova.com
Country
China
ProdList
4195
Advantage
58

1239358-85-0, NS-018 (hydrochloride)Related Search:


  • NS-018 (hydrochloride)
  • ILGINATINIB HYDROCHLORIDE (NS-018 HYDROCHLORIDE)
  • Ilginatinib hydrochloride
  • Tyk2,Ilginatinib,JAK1,JAK,JAK2,Inhibitor,bioavailable,NS018,NS-018,orally,inhibit,Janus kinase,JAK3,Ilginatinib hydrochloride,NS 018
  • Ilginatinibhydrochloride(NS-018 HCI)
  • Ilginatinib hydrochloride, 10 mM in DMSO
  • Ilginatinib (NS-018) hydrochloride
  • (S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine hydrochloride
  • 1239358-85-0
  • C21H21ClFN7