2378581-37-2
Chemical Structure
SIAIS056
- CAS No.: 2378581-37-2
- Formula:C35H34ClN9O5S2
- Molecular Weight:760.28
InChIKey: QOGZTNFOSUHSAL-UHFFFAOYSA-N
SMILES: O=C(C1=CN=C(NC2=CC(N3CCN(CC3)CCSC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=NC(C)=N2)S1)NC7=C(C)C=CC=C7Cl
Biological Activity: SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research[1][2].
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SIAIS056 | SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research. | |||||||||||||||||||||
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- [1]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
- [2]. Kang CH, et al. Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC). Biochem Biophys Res Commun. 2018 Oct 28;505(2):542-547. [Content Brief]
Keywords
