| Identification | Back Directory | [Name]
WP1066 | [CAS]
857064-38-1 | [Synonyms]
WP1066
CS-604
WP1066, >=99%
WP1066/WP-1066
WP1066 USP/EP/BP
STAT Inhibitor III
WP1066; WP 1066;WP-1066
wp1066(STAT Inhibitor III)
Stat3 Inhibitor III, WP1066
WP1066, 98%, a novel inhibitor of JAK2 and STAT3
(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide
(E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide
2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-, (2E)-
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 | [Molecular Formula]
C17H14BrN3O | [MDL Number]
MFCD12912450 | [MOL File]
857064-38-1.mol | [Molecular Weight]
356.217 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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.1 It also induces apoptosis in U87-MG (IC50 = 5.6 μM) and U373-MG (IC50 = 3.7 μM) cells.1 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.2,3 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.4,5 | [Uses]
Cell permeable STAT3 inhibitor. Activates Bax. Shows potent anticancer effect on malignant glioma cells. Induces apoptosis and inhibits the growth of tumors. Acts as a potent immune adjuvant by upregulating CD80 and CD86 and inducing proliferation of effector T cells. | [in vivo]
WP1066 (30 mg/kg, o.g.) exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment[2]. | [target]
JAK2 | [IC 50]
JAK2; STAT3 | [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 |
|
|