For research use only. Not for therapeutic Use.
TK216(CAT: I017630) is a potent, orally active inhibitor of E26 transformation-specific (ETS) transcription factors, developed to target the oncogenic fusion protein EWS-FLI1. It directly binds EWS-FLI1, disrupting its interactions with RNA helicase A and inhibiting downstream transcriptional activity. TK216 demonstrates strong anticancer activity, inducing apoptosis in DLBCL cell lines and inhibiting proliferation in Ewing sarcoma A4573 cells in a dose-dependent manner. It shows IC₅₀ values of 0.363 μM (HL-60 AML) and 0.152 μM (TMD-8 DLBCL). In vivo, oral TK216 (100 mg/kg, twice daily) significantly suppresses tumor growth in xenograft models, highlighting its promise as a targeted oncology therapeutic.
| CAS Number | 1903783-48-1 |
| Synonyms | 4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one |
| Molecular Formula | C19H15Cl2NO3 |
| Purity | ≥95% |
| IUPAC Name | 4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one |
| InChI | InChI=1S/C19H15Cl2NO3/c20-13-7-8-14(21)17-16(13)19(25,18(24)22-17)9-15(23)12-5-3-11(4-6-12)10-1-2-10/h3-8,10,25H,1-2,9H2,(H,22,24) |
| InChIKey | ZWHNLSHDLKIXOG-UHFFFAOYSA-N |
| SMILES | C1CC1C2=CC=C(C=C2)C(=O)CC3(C4=C(C=CC(=C4NC3=O)Cl)Cl)O |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
