ChemicalBook > CAS DataBase List > NS-018 (hydrochloride)

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
More
Less

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
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

More
Less

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
More
Less

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

More
Less

NS-018 (hydrochloride) Suppliers

China 28 United States 5 Global 33
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
2965
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
32469
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
Shanghai Luofa Biochemical Technology Co., Ltd.
Tel
021-51111890 15317326293
Email
sales@molnova.com
Country
China
ProdList
4195
Advantage
58
ShangHai ChuanQian Chemcial Technique Centre
Tel
15869524721
Email
3525679403@qq.com
Country
China
ProdList
4998
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