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.

in vivo

target

JAK2

IC 50

JAK2; STAT3

References

[1] Discovery of WP1066, a novel Stat3/c-myc inhibitor with potent antitumor activity against human melanoma in vitro and in vivo
[2] A IWAMARU. A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo[J]. Oncogene, 2006, 26 17: 2435-2444. DOI:10.1038/sj.onc.1210031
[3] ALESSANDRA FERRAJOLI. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells.[J]. Cancer research, 2007, 67 23: 11291-11299. DOI:10.1158/0008-5472.can-07-0593
[4] LING-YUAN KONG. 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.[J]. Clinical Cancer Research, 2008, 14 18: 5759-5768. DOI:10.1158/1078-0432.ccr-08-0377
[5] LING-YUAN KONG. A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells.[J]. Cancer Immunology, Immunotherapy, 2009, 58 7: 1023-1032. DOI:10.1007/s00262-008-0618-y
[6] CHAOYA MA. Stat3 inhibitor abrogates the expression of PD-1 ligands on lymphoma cell lines.[J]. Journal of Clinical and Experimental Hematopathology, 2017, 57 1: 21-25. DOI:10.3960/jslrt.17006

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