420151
JAK2 Inhibitor IX, WP1193
Synonym(s):
JAK2 Inhibitor IX, WP1193, ( S, E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(cyclopropyl(phenyl)methyl)acrylamide
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About This Item
Empirical Formula (Hill Notation):
C19H16BrN3O
Molecular Weight:
382.25
UNSPSC Code:
12352200
Assay
≥95% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
brown
solubility
methanol: 1 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable tyrphostin WP1130 (Cat. No. 681685) analog that inhibits JAK2 kinase activity (by >90% at 2.5 µM in in vitro kinase assays) and effectively suppresses JAK2-dependent STAT3 Tyr705 phosphorylation in murine melanoma B16 and human GSC (glioma stem-like cell) cultures (5 µM), as well as JAK2-dependent Bcr-Abl Tyr177 phosphorylation in primary human CML PBMCs, Imatinib/STI571-sensitive 32DP210, and IM-resistant Ba/F3-T315I murine leukemia lines (10 µM). Reported to inhibit the growths of IM-resistant K562-R and T315I+ 32D in murine leukemia models (30 mg/kg via i.p.; q.o.d.), as well as synergize with INF-α in suppressing B16 blood-to-lung metastasis and eliminating LMD (lentiginous melanocytic dysplasia) in mice died from established B26-derived brain tumor (30 mg WP1130/kg via o.g./oral gavage) in vivo.
A cell-permeable tyrphostin WP1130 (Cat. No. 681685) analog that inhibits JAK2 kinase activity (by >90% at 2.5 µM in in vitro kinase assays) and effectively suppresses JAK2-dependent STAT3 Tyr705 phosphorylation in murine melanoma B16 and human GSC (glioma stem-like cell) cultures (5 µM), as well as JAK2-dependent Bcr-Abl Tyr177 phosphorylation in primary human CML PBMCs, Imatinib/STI571-sensitive 32DP210, and IM-resistant Ba/F3-T315I murine leukemia lines (10 µM). Reported to inhibit the growths of IM-resistant K562-R and T315I+ 32D in murine leukemia models (30 mg/kg via i.p.; q.o.d.), as well as synergize with INF-α in suppressing B16 blood-to-lung metastasis and eliminating LMD (lentiginous melanocytic dysplasia) in mice died from established B26-derived brain tumor (30 mg WP1130/kg via o.g./oral gavage) in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JAK2
JAK2
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Sai, K., et al. 2012. J. Neurooncol.107, 487.
Samanta, A., et al. 2011. Leukemia25, 463.
Kong, L.Y., et al. 2010. Clin. Cancer Res.16, 2550.
Samanta, A., et al. 2011. Leukemia25, 463.
Kong, L.Y., et al. 2010. Clin. Cancer Res.16, 2550.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Certificates of Analysis (COA)
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