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JAK2 Inhibitor V, Z3 (Synonyms: Z3; NSC 42834;1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-)

Catalog No.GC13826

A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK

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JAK2 Inhibitor V, Z3 Chemical Structure

Cas No.: 195371-52-9

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10mM (in 1mL DMSO)
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5mg
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10mg
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50mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

NSC 42834 (JAK2 Inhibitor V) selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. NSC 42834 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The NSC 42834-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, NSC 42834 inhibited the growth of hematopoietic progenitor cells isolated from the bone marrow of an essential thrombocythemia patient harboring the Jak2-V617F mutation and a polycythemia vera patient carrying a Jak2-F537I mutation.

References:
[1]. Jacqueline Sayyah, Andrew Magis, David A. Ostrov, et al. Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth . Mol Cancer Ther 2008;7(8):2308-18.
[2]. Jacqueline Sayyah, Peter P. Sayeski. Jak2 inhibitors: Rationale and role as therapeutic agents in hematologic malignancies. Current Oncology Reports. 2009, 11(2): 117-124.
[3]. Ehab Atallah , Srdan Verstovsek . Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms. Expert Review of Anticancer Therapy. 2009,9 (5):663-670.

Chemical Properties

Cas No. 195371-52-9 SDF
Synonyms Z3; NSC 42834;1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-
Chemical Name 2-methyl-1-phenyl-4-(pyridin-2-yl)-2-(2-(pyridin-2-yl)ethyl)butan-1-one
Canonical SMILES CC(CCC1=CC=CC=N1)(C(C2=CC=CC=C2)=O)CCC3=CC=CC=N3
Formula C23H24N2O M.Wt 344.45
Solubility DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.9032 mL 14.5159 mL 29.0318 mL
5 mM 0.5806 mL 2.9032 mL 5.8064 mL
10 mM 0.2903 mL 1.4516 mL 2.9032 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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