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JAK2 Inhibitor V, Z3

Jak2 tyrosine kinase inhibitor CAS# 195371-52-9

JAK2 Inhibitor V, Z3

Catalog No. BCC1667----Order now to get a substantial discount!

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JAK2 Inhibitor V, Z3: 5mg $276 In Stock
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Chemical structure

JAK2 Inhibitor V, Z3

3D structure

Chemical Properties of JAK2 Inhibitor V, Z3

Cas No. 195371-52-9 SDF Download SDF
PubChem ID 238484 Appearance Powder
Formula C23H24N2O M.Wt 344.45
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Z3
Solubility DMSO : ≥ 100 mg/mL (290.32 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-methyl-1-phenyl-4-pyridin-2-yl-2-(2-pyridin-2-ylethyl)butan-1-one
SMILES CC(CCC1=CC=CC=N1)(CCC2=CC=CC=N2)C(=O)C3=CC=CC=C3
Standard InChIKey SETYDCSRABYHSW-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of JAK2 Inhibitor V, Z3

DescriptionNSC 42834(JAK2 Inhibitor V, Z3), 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. IC50 value: Target: Jak2; Jak2-V617F Z3 selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. Z3 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The Z3-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, Z3 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.

JAK2 Inhibitor V, Z3 Dilution Calculator

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JAK2 Inhibitor V, Z3 Molarity Calculator

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Preparing Stock Solutions of JAK2 Inhibitor V, Z3

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9032 mL 14.5159 mL 29.0318 mL 58.0636 mL 72.5795 mL
5 mM 0.5806 mL 2.9032 mL 5.8064 mL 11.6127 mL 14.5159 mL
10 mM 0.2903 mL 1.4516 mL 2.9032 mL 5.8064 mL 7.2579 mL
50 mM 0.0581 mL 0.2903 mL 0.5806 mL 1.1613 mL 1.4516 mL
100 mM 0.029 mL 0.1452 mL 0.2903 mL 0.5806 mL 0.7258 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on JAK2 Inhibitor V, Z3

Z3 is a novel specific inhibitor of Jak2 tyrosine kinase. Z3 inhibited Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

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Description

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.

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