GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kgamma, PI3Kalpha and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110alpha and p110gamma with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) [1].
Molekulargewicht:
1073.31
Formel:
C56H72N12O8S
Target-Kategorie:
Apoptosis,mTOR,PI3K,PROTACs
Anwendungsbeschreibung:
MCE Product type: Reference compound1
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