1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

NS-018 maleate 

Cat. No.: HY-19631
Handling Instructions

NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470 nM in Ba/F3-JAK2V617F cells, have30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2.

For research use only. We do not sell to patients.
NS-018 maleate Chemical Structure

NS-018 maleate Chemical Structure

CAS No. : 1354799-87-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $389 In-stock
1 mg $150 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of NS-018 maleate:

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470 nM in Ba/F3-JAK2V617F cells, have30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2. target: JAK2 IC 50: 470 nM In vitro: NS-018 suppressed the phosphorylation of STAT3 in colony-forming cells. NS-018 inhibited Src-family kinases. NS-018 showed potent antiproliferative activity against cell lines expressing a constitutively activated JAK2. NS-018 also markedly reduced splenomegaly and prolonged the survival of mice inoculated with Ba/F3 cells harboring JAK2V617F. In vivo: NS-018 significantly reduced leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improved nutritional status, and prolonged survival in JAK2V617F transgenic mice. NS-018 also inhibited erythroid colony formation in JAK2V617F transgenic mice at significantly lower concentrations than in WT mice.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01423851 NS Pharma, Inc. Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis June 2011 Phase 1|Phase 2
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References
Molecular Weight

505.5

Formula

C₂₅H₂₄FN₇O₄

CAS No.

1354799-87-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
NS-018 maleate
Cat. No.:
HY-19631
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