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
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 195371-52-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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