Cas No.: | 857064-38-1 |
Chemical Name: | 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2E-propenamide |
Synonyms: | wp1066, wp 1066,wp-1066 |
SMILES: | C[C@@H](C1=CC=CC=C1)NC(=O)/C(=C/C2=NC(=CC=C2)Br)/C#N |
Formula: | C17H14BrN3O |
M.Wt: | 356.2 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3. |
In Vivo: | WP1066 (30 mg/kg, o.g.)does not further enhance the therapeutic effects of cyclophosphamide on pulmonary melanoma lesions, enhance the therapeutic effects of cyclophosphamide against CNS melanoma, or further enhance immune-mediated cytotoxic effects of CTX in C57BL/6J mice. WP1066 exerts an additive effect to CTX inhibition of the p-STAT3 pathway within the tumor microenvironment[2]. |
In Vitro: | WP1066 markedly inhibits the growth of HEL cells in a dose-dependent manner. The IC50 value for inhibition of the proliferation of HEL cells is 2.3 μM. WP1066 inhibits the growth of human HEL cells carrying the JAK2 V617F mutant isoform[1]. Blockade of p-STAT3 with WP1066 enhances the cytotoxic effects of CTX on the tumor. The IC50 doses of WP1066 for B16 cells is 2.43 µM (0.865 µg/mL)[2]. WP1066 inhibits AML blast colony-forming cell proliferation, suppresses normal BM progenitor proliferation at increased concentrations, and inhibits AML colony-forming cell proliferation[3]. |