Description
WP1130 can inhibit Bcr/Abl with IC50 of 1.8 uM.
Storage
2 years at -20 centigrade
Molecular Formula
C19H18BrN3O
Chemical Name
(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
Solubility
DSMO 77 mg/mL Water
In vitro
WP1130, is a second-generation tyrphostin derivative (degrasyn) discovered during screens for AG490-like molecules that suppress IL-6 and IL-3 activation of Stat molecules. WP1130 can reduce cytokine-stimulated Stat activation through the rapid down-regulation of upstream Jak kinases In CML cells, WP1130 induced down-regulation of Bcr/Abl protein without affecting bcr-abl mRNA levels. WP1130 speci?cally and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. WP1130 promotes Mcl-1 degradation and increases tumor cell sensitivity to chemotherapies. The combination of WP1130 and ABT-737, a well-documented Bcl-xL inhibitor, demonstrated a chemotherapeutic synergy and promoted apoptosis in different tumor cells.
In vivo
WP1130 suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice.
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