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Haoyuan Chemexpress Co., Ltd.
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| Products Intro: |
Product Name:NS-018 (hydrochloride)
CAS:1239358-85-0
Purity:>98% Package:3500RMB/5mg
|
| Company Name: |
MedChemexpress LLC
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| Tel: |
021-58955995 |
| Email: |
sales@medchemexpress.cn |
| Products Intro: |
Product Name:NS-018 (hydrochloride)
CAS:1239358-85-0
Purity:>98% Package:3500RMB/5mg
|
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| | NS-018 (hydrochloride) Basic information |
| Product Name: | NS-018 (hydrochloride) | | Synonyms: | 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) | | CAS: | 1239358-85-0 | | MF: | C21H21ClFN7 | | MW: | 425.8897432 | | EINECS: | | | Product Categories: | | | Mol File: | 1239358-85-0.mol |  |
| | NS-018 (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : ≥ 35 mg/mL (82.18 mM) | | form | Solid | | color | Light yellow to yellow |
| | NS-018 (hydrochloride) Usage And Synthesis |
| 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]. | | 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 |
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