| Identification | Back Directory | [Name]
TK216 | [CAS]
1903783-48-1 | [Synonyms]
TK216
4,7-dichloro-3-(2-(4-cyclopropylphenyl)-2-oxoethyl)-3-hydroxyindolin-2-one
2H-Indol-2-one, 4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-1,3-dihydro-3-hydroxy- | [Molecular Formula]
C19H15Cl2NO3 | [MOL File]
1903783-48-1.mol | [Molecular Weight]
376.23 |
| Chemical Properties | Back Directory | [Boiling point ]
614.0±55.0 °C(Predicted) | [density ]
1.473±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥ 250 mg/mL (664.49 mM) | [form ]
Solid | [pka]
10.40±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor[1]. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity[2]. | [in vivo]
TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition of the TMD-8 xenograft model[1].
| Animal Model: | NOD-Scid mice subcutaneously inoculated with TMD8 cells[1] | | Dosage: | 100 mg/kg | | Administration: | PO; twice daily for 13 days | | Result: | Resulted in tumor growth inhibition.
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| [storage]
Store at -20°C | [References]
[1] Spriano F, et al. The ETS Inhibitors YK-4-279 and TK-216 Are Novel Antilymphoma Agents. Clin Cancer Res. 2019 Aug 15;25(16):5167-5176. DOI:10.1158/1078-0432.CCR-18-2718
[2] Brian Lannutti, et al. Uses of indolinone compounds. US10159660B2. |
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