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WP 1066
- Optical Purity: Optically pure
- Soluble in DMSO and EtOH
- MF: C17H14BrN3O
- MW: 356.22
Description
Potent inhibitor of JAK2 and STAT3 activity (IC50 values 2.3 µM and 5.6 µM, respectively) that showed selective cytotoxicity toward malignant glioma U87-MG and U373-MG cells at much lower doses than its analogue AG 490 (Axon 1378). Furthermore, WP1066 selectively induces apoptosis in malignant glioma cells by downregulating antiapoptotic proteins (Bcl-XL, Mcl-1 and c-myc) and activating Bax, and significantly inhibited the growth of subcutaneous tumors generated from U87-MG cells in mice.
More Information
| Parent CAS No. | 857064-38-1 |
|---|---|
| Chemical Name | (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide |
| SMILES | C(N[C@H](C1=CC=CC=C1)C)(=O)/C(/C#N)=C/C1=NC(Br)=CC=C1 |&1:2,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1 |
| InChiKey | VFUAJMPDXIRPKO-LQELWAHVSA-N |
| CID | 11210478 |
| Short Description | JAK2/STAT3 inhibitor |
References
- A. Iwamaru et al. A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both in vitro and in vivo. Oncogene. 2007, 26, 2435-2444.
- M.A. Hatiboglu et al. The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models. Int. J. Cancer. 2012, 131, 8-17.
- S. Verstovsek et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin. Cancer Res. 2008, 14, 788-796.
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