WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H528802
CAS#: 1354799-87-3 (maleate)
Description: Ilginatinib, also known as NS-018, is a selective JAK2 inhibitor. Ilginatinib preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. NS-018 suppressed the phosphorylation of STAT3 in colony-forming cells from MDS patients. NS-018 reduces myeloma cell proliferation and suppresses osteolysis through inhibition of the JAK2 and Src signaling pathways.
Hodoodo Cat#: H528802
Name: Ilginatinib maleate
CAS#: 1354799-87-3 (maleate)
Chemical Formula: C25H24FN7O4
Exact Mass: 0.00
Molecular Weight: 505.510
Elemental Analysis: C, 59.40; H, 4.79; F, 3.76; N, 19.40; O, 12.66
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Related CAS #: 1239358-86-1 (free base) 1239358-85-0 (HCl) 1354799-87-3 (maleate)
Synonym: NS-018; NS018; NS 018; NS-018 maleate; Ilginatinib maleate;
IUPAC/Chemical Name: (S)-N2-(1-(4-fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate
InChi Key: OVAGJAAQMBYZDS-FXSDFHGDSA-N
InChi Code: InChI=1S/C21H20FN7.C4H4O4/c1-14(15-3-5-18(22)6-4-15)26-19-9-16(17-11-25-29(2)13-17)10-20(27-19)28-21-12-23-7-8-24-21;5-3(6)1-2-4(7)8/h3-14H,1-2H3,(H2,24,26,27,28);1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-;/m0./s1
SMILES Code: CN1N=CC(C2=CC(N[C@H](C3=CC=C(F)C=C3)C)=NC(NC4=NC=CN=C4)=C2)=C1.O=C(O)/C=C\C(O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 505.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Verstovsek S, Talpaz M, Ritchie E, Wadleigh M, Odenike O, Jamieson C, Stein B, Uno T, Mesa RA. A phase I, open-label, dose-escalation, multicenter study of the JAK2 inhibitor NS-018 in patients with myelofibrosis. Leukemia. 2017 Feb;31(2):393-402. doi: 10.1038/leu.2016.215. PubMed PMID: 27479177; PubMed Central PMCID: PMC5292677.
2: Kuroda J, Kodama A, Chinen Y, Shimura Y, Mizutani S, Nagoshi H, Kobayashi T, Matsumoto Y, Nakaya Y, Tamura A, Kobayashi Y, Naito H, Taniwaki M. 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. PubMed PMID: 24679585.
3: Nakaya Y, Shide K, Naito H, Niwa T, Horio T, Miyake J, Shimoda K. Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer J. 2014 Jan 10;4:e174. doi: 10.1038/bcj.2013.73. PubMed PMID: 24413068; PubMed Central PMCID: PMC3913942.
4: Nakaya Y, Shide K, Niwa T, Homan J, Sugahara S, Horio T, Kuramoto K, Kotera T, Shibayama H, Hori K, Naito H, Shimoda K. 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. PubMed PMID: 22829185; PubMed Central PMCID: PMC3255248.
5: Furqan M, Mukhi N, Lee B, Liu D. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark Res. 2013 Jan 16;1(1):5. doi: 10.1186/2050-7771-1-5. PubMed PMID: 24252238; PubMed Central PMCID: PMC3776247.
6: Rosenthal A, Mesa RA. Janus kinase inhibitors for the treatment of myeloproliferative neoplasms. Expert Opin Pharmacother. 2014 Jun;15(9):1265-76. doi: 10.1517/14656566.2014.913024. Review. PubMed PMID: 24766055.
7: Tam CS, Verstovsek S. Investigational Janus kinase inhibitors. Expert Opin Investig Drugs. 2013 Jun;22(6):687-99. doi: 10.1517/13543784.2013.774373. Review. PubMed PMID: 23432430.