2353494-84-3
Chemical Structure
SIAIS117
- CAS No.: 2353494-84-3
- Formula:C57H76ClN10O7PS
- Molecular Weight:1111.77
IUPAC Name: (8S,10S)-8-(2-bromoacetyl)-6,8,10,11-tetrahydroxy-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione
InChIKey: DYUJLNPTOOBZBB-CCXZOALNSA-N
SMILES: COC(C=C1N(CC2)CCC2NC(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)=O)=O)=O)=C(C=C1)NC6=NC=C(Cl)C(NC7=C(C=CC=C7)P(C)(C)=O)=N6
Biological Activity: SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors[1].
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SIAIS117 | SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors. | |||||||||||||||||||||
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