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SIAIS056

SKU: orb3177251

Description

SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner in K562 cells and reduces the phosphorylation levels of BCR-ABL and its downstream molecules, STAT5 and CRKL. SIAIS056 can induce the degradation of various clinically relevant BCR-ABL resistant mutants and exhibits antiproliferative activity against K562 and 32D-BCR-ABL cells. Additionally, it can cause significant tumor regression in K562 xenograft models and is applicable for leukemia research.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

Key Properties

CAS Number2378581-37-2
MW760.29
FormulaC35H34ClN9O5S2
SMILESO=C(NC=1C(Cl)=CC=CC1C)C=2SC(=NC2)NC=3N=C(N=C(C3)N4CCN(CCSC5=CC=CC=6C(=O)N(C(=O)C56)C7C(=O)NC(=O)CC7)CC4)C
TargetPROTACs,Bcr-Abl

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information