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NS-018 (maleate)

Product Name
NS-018 (maleate)
CAS No.
1354799-87-3
Chemical Name
NS-018 (maleate)
Synonyms
NS-018 (maleate);Ilginatinib maleate;Ilginatinib (NS-018) maleate;NS018 MALEATE;ILGINATINIB MALEATE;Ilginatinib maleate, 10 mM in DMSO;ILGINATINIB (MALEATE) (NS-018 (MALEATE));(S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate;Inhibitor,JAK3,NS 018,inhibit,JAK2,Ilginatinib,bioavailable,NS018,orally,Ilginatinib maleate,NS-018,JAK1,Janus kinase,JAK,Tyk2
CBNumber
CB03137709
Molecular Formula
C25H24FN7O4
Formula Weight
505.5009632
MOL File
1354799-87-3.mol
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NS-018 (maleate) Property

storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 30 mg/mL (59.35 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-5784
Product name
Ilginatinibmaleate
Purity
97.04%
Packaging
5mg
Price
$285
Updated
2021/12/16
ChemScene
Product number
CS-5784
Product name
Ilginatinibmaleate
Purity
97.04%
Packaging
10mg
Price
$395
Updated
2021/12/16
ChemScene
Product number
CS-5784
Product name
Ilginatinibmaleate
Purity
97.04%
Packaging
25mg
Price
$580
Updated
2021/12/16
ChemScene
Product number
CS-5784
Product name
Ilginatinibmaleate
Purity
97.04%
Packaging
50mg
Price
$870
Updated
2021/12/16
ChemScene
Product number
CS-5784
Product name
Ilginatinibmaleate
Purity
97.04%
Packaging
100mg
Price
$1250
Updated
2021/12/16
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NS-018 (maleate) Chemical Properties,Usage,Production

Uses

Ilginatinib maleate (NS-018 maleate) 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).

Biological Activity

Ilginatinib maleate (NS-018 maleate) is a highly potent, orally available JAK2 inhibitor with IC50 of 0.72 nM, 46-fold selectivity for JAK1 (IC50, 33 nM) and 54-fold for JAK3 ( IC50, 39 nM), and 22 times that of Tyk2 (IC50, 22 nM).

in vivo

Ilginatinib maleate (NS-018 maleate) (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.

target

JAK2

0.72 nM (IC 50 )

Tyk2

22 nM (IC 50 )

JAK1

33 nM (IC 50 )

JAK3

39 nM ( IC 50 )

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. DOI:10.1038/bcj.2011.29
[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. DOI:10.1016/j.leukres.2014.03.001

NS-018 (maleate) Preparation Products And Raw materials

Raw materials

Preparation Products

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NS-018 (maleate) Suppliers

China 27 United States 5 Global 32
Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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info@efebio.com
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China
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Shanghai Chaolan Chemical Technology Center
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021-QQ：65489617 15618227136
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1354799-87-3, NS-018 (maleate)Related Search:


  • NS-018 (maleate)
  • Ilginatinib maleate
  • NS018 MALEATE;ILGINATINIB MALEATE
  • ILGINATINIB (MALEATE) (NS-018 (MALEATE))
  • Inhibitor,JAK3,NS 018,inhibit,JAK2,Ilginatinib,bioavailable,NS018,orally,Ilginatinib maleate,NS-018,JAK1,Janus kinase,JAK,Tyk2
  • (S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate
  • Ilginatinib maleate, 10 mM in DMSO
  • Ilginatinib (NS-018) maleate
  • 1354799-87-3