JAK2 INHIBITOR X FLLL32 (C15-1305-008)

General description

A cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC₅₀ >100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC₅₀ = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.

A cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC₅₀ >100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC₅₀ = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
JAK2

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Wu, J., et al. 2014. Oncogene33,173.
Onimoe, G., et al. 2012. Invest. New Drugs30, 916.
Li, L., et al. 2010. Cancer Res.70, 2445.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 464.55. Empirical Formula: C₂₈H₃₂O₆. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 5 . μ. M IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.