Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
WP1130
Cat No.
CEI-0264
Description
WP1130 can inhibit Bcr/Abl with IC50 of 1.8 uM.
CAS No.
856243-80-6
Molecular Weight
384.27
Purity
>99%
Storage
2 years at -20 centigrade
Targets
Bcr-Abl
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.
Download
Download Datasheet