(+)-YK-4-279


CAS No. : 1261038-93-0

(+)-YK-4-279,1261038-93-0
Product Details
Cat No:M030970
Synonyms:4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-(3R)-2H-indol-2-one
Molecular Formula:C17H13Cl2NO4
Molecular Weight:366.194
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Assay:≥98%
Appearance:A crystalline solid
Cat No:M030970
Cas No:1261038-93-0
Product-Name:(+)-YK-4-279
IUPAC Name:(3R)-4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
InChI:InChI=1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22)/t17-/m1/s1
InChIKey:HLXSCTYHLQHQDJ-QGZVFWFLSA-N
SMILES:COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O
Ewing’s sarcoma is characterized by the formation of an oncogenic fusion protein, EWS-FLI1, which binds to RNA helicase central to disease. YK-4-279 binds to EWS-FLI1 (Kd = 9.48 μM), blocking the interaction of EWS-FLI1 and RNA helicase and driving apoptosis in Ewing’s sarcoma family tumors. Through these effects, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts. Importantly, it is effective in Ewing’s sarcoma cells, both in vitro and in vivo, that are chemotherapy-resistant. YK-4-279 also binds the ETS transcription factors ERG and ETV1 (Kd = 11.7 and 17.4, respectively), which form fusion proteins that contribute to some types of prostate cancer. (+)-YK-4-279 is a highly purified enantiomer of YK-4-279. Its properties have not been characterized.
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