NS-018
- Product Name
- NS-018
- CAS No.
- 1239358-86-1
- Chemical Name
- NS-018
- Synonyms
- NS-018;Ilginatinib;NS018;ILGINATINIB;ILGINATINIB (NS-018);Ilginatinib, 10 mM in DMSO;JAK3,Janus kinase,Inhibitor,NS 018,JAK,JAK2,orally,Tyk2,NS018,Ilginatinib,inhibit,JAK1,bioavailable;2,6-Pyridinediamine, N2-[(1S)-1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-2-pyrazinyl-;N2-[(1S)-1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine
- CBNumber
- CB83067013
- Molecular Formula
- C21H20FN7
- Formula Weight
- 389.43
- MOL File
- 1239358-86-1.mol
NS-018 Property
- Boiling point:
- 574.1±50.0 °C(Predicted)
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 34 mg/mL (87.31 mM)
- form
- Solid
- pka
- 2.43±0.10(Predicted)
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-5358
- Product name
- Ilginatinib
- Purity
- 99.15%
- Packaging
- 5mg
- Price
- $285
- Updated
- 2021/12/16
- Product number
- CS-5358
- Product name
- Ilginatinib
- Purity
- 99.15%
- Packaging
- 10mg
- Price
- $395
- Updated
- 2021/12/16
- Product number
- CS-5358
- Product name
- Ilginatinib
- Purity
- 99.15%
- Packaging
- 25mg
- Price
- $580
- Updated
- 2021/12/16
- Product number
- orb611581
- Product name
- NS-018
- Packaging
- 100mg
- Price
- $1060.8
- Updated
- 2021/12/16
- Product number
- CS-5358
- Product name
- Ilginatinib
- Purity
- 99.15%
- Packaging
- 100mg
- Price
- $1250
- Updated
- 2021/12/16
NS-018 Chemical Properties,Usage,Production
Uses
Ilginatinib (NS-018) 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 (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[1].
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
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 Preparation Products And Raw materials
Raw materials
Preparation Products
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