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| 25mg |
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Purity: ≥98%
NSC 42834 (also known as NSC42834; JAK2 Inhibitor V) is a novel, potent and specific inhibitor of JAK2 which inhibits JAK2-V617F and JAK2-WT autophosphorylation in a dose-dependent manner with IC50 values between 10 and 30 µM. It was not cytotoxic to cells at concentrations that inhibited kinase activity.
| ln Vitro |
Tyk2 and c-Src kinase function are unaffected by NSC 42834 (JAK2 inhibitor V), which specifically suppresses Jak2 kinase activity. The proliferation of the human erythroleukemia cell line HEL 92.1.7, which expresses Jak2-V617F, is greatly inhibited by NSC 42834. Significant cell cycle arrest and lower levels of Jak2 and STAT3 tyrosine phosphorylation were linked to the NSC 42834-mediated reduction in cell proliferation. Lastly, hematopoietic progenitor cells derived from the bone marrow of individuals with polycythemia vera who have the Jak2-F537I mutation and essential thrombocythemia who harbor the Jak2-V617F mutation are inhibited in growth by NSC 42834.
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| 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. |
| Molecular Formula |
C23H24N2O
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|---|---|
| Molecular Weight |
344.449465751648
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| CAS # |
195371-52-9
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| SMILES |
O=C(C(CCC1=CC=CC=N1)(CCC2=NC=CC=C2)C)C3=CC=CC=C3
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| InChi Key |
SETYDCSRABYHSW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24N2O/c1-23(15-13-20-11-5-7-17-24-20,16-14-21-12-6-8-18-25-21)22(26)19-9-3-2-4-10-19/h2-12,17-18H,13-16H2,1H3
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| Chemical Name |
2-methyl-1-phenyl-4-(pyridin-2-yl)-2-(2-(pyridin-2-yl)ethyl)butan-1-one
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| Synonyms |
NSC 42834; NSC42834; Janus-Associated Kinase Inhibitor V; NSC-42834; Z3. JAK2 Inhibitor V.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~290.32 mM)
Ethanol : ~100 mg/mL (~290.32 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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