SIAIS117
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer[1].
Product Specifications
CAS Number
[2353494-84-3]
UNSPSC
12352005
Target
Anaplastic lymphoma kinase (ALK) ; PROTACs
Type
Reference compound
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/siais117.html
Solubility
10 mM in DMSO
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
Molecular Formula
C57H76ClN10O7PS
Molecular Weight
1111.77
References & Citations
[1]Sun N, Ren C, Kong Y, et al. Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance. Eur J Med Chem. 2020;193:112190.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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