WP1066 Chemical Properties

Melting point:

90-93oC

Boiling point:

569.9±50.0 °C(Predicted)

Density 

1.425

storage temp. 

+2C to +8C

solubility 

Soluble in DMSO (up to at least 25 mg/ml)

form 

Off-white solid

pka

11.00±0.46(Predicted)

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety Information

HS Code 

29333990

WP1066 Usage And Synthesis

Description

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 μM. It also induces apoptosis in U87-MG (IC₅₀ = 5.6 μM) and U373-MG (IC₅₀ = 3.7 μM) cells. WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.

Uses

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells.

target

JAK2

References

1) Kong?et al.?(2005),?Discovery of WP1066, a novel Stat3/c-myc inhibitor with potent antitumor activity against human melanoma in vitro and in vivo;?Cancer Res.?65?1387 2) Iwamaru?et al.?(2007),?A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both invitro and in vivo;?Oncogene?26?2435 3) Ferraioli?et al.?(2007),?WP1066 Disrupts Janus Kinase-2 and Induces Caspase-Dependent Apoptosis in acute Myelogenous Leukemia Cells;?Cancer Res.?67?11291 4) Kong,?et al.?(2008),?A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells;?Clin. Cancer Res.?14?5759 5) Kong,?et al.?(2009),?A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells;?Cancer Immunol. Immunother.?58?1023 6) Ma,?et al.?(2017),?Stat3 inhibitor abrogates the expression of PD-1 ligands on Lymphoma cell lines;?J. Clin. Exp. Hematop.?57?21

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