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JAK2 Inhibitor V

Cat. No. M3735
JAK2 Inhibitor V Structure
Synonym:

NSC 42834, Z3

Size Price Availability Quantity
5mg USD 330 In stock
10mg USD 520 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Z3 (NSC 42834) 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 (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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 344.45
Formula C23H24N2O
CAS Number 195371-52-9
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms.
Atallah E, et al. Expert Rev Anticancer Ther. 2009 May;9(5):663-70. PMID: 19445582.

Jak2 inhibitors: rationale and role as therapeutic agents in hematologic malignancies.
Sayyah J, et al. Curr Oncol Rep. 2009 Mar;11(2):117-24. PMID: 19216843.

Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth.
Sayyah J, et al. Mol Cancer Ther. 2008 Aug;7(8):2308-18. PMID: 18723478.

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JANEX-1

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JAK2 Inhibitor V, NSC 42834, Z3 supplier, JAK, inhibitors

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