NSC 42834

Modify Date: 2024-01-12 12:30:39

NSC 42834 Structure
NSC 42834 structure
Common Name NSC 42834
CAS Number 195371-52-9 Molecular Weight 344.449
Density 1.1±0.1 g/cm3 Boiling Point 520.4±50.0 °C at 760 mmHg
Molecular Formula C23H24N2O Melting Point N/A
MSDS N/A Flash Point 263.0±36.5 °C

 Use of NSC 42834


NSC 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-V617FZ3 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.

 Names

Name 2-methyl-1-phenyl-4-pyridin-2-yl-2-(2-pyridin-2-ylethyl)butan-1-one
Synonym More Synonyms

 NSC 42834 Biological Activity

Description NSC 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-V617FZ3 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.
Related Catalog
Target

JAK2-WT:15 μM (IC50)

JAK2-V617F:28 μM (IC50)

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 & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 520.4±50.0 °C at 760 mmHg
Molecular Formula C23H24N2O
Molecular Weight 344.449
Flash Point 263.0±36.5 °C
Exact Mass 344.188873
PSA 42.85000
LogP 4.06
Appearance of Characters light yellow oil
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.586
Storage condition -20℃

 Safety Information

 Synonyms

1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-
2-methyl-1-phenyl-4-(pyridin-2-yl)-2-[2-(pyridin-2-yl)ethyl]butan-1-one
2-Methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-1-butanone
JAK2 Inhibitor V,Z3
HMS3092H09
NSC 42834
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