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TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $313 | In Stock | |
50 mg | $538 | In Stock | |
100 mg | $778 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
Description | TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity. |
In vitro | In DLBCL cell lines, TK216 (500 nM; for 24-72 hours) induces apoptosis [1]. TK216 (0.03, 0.06, 0.125, 0.25, 0.5 μM) results in a dose-dependent inhibition of proliferation in Ewing Sarcoma A4573 cell line[1]. In DLBCL cell lines,TK216 (0.1, 0.3, 1 μM) induces apoptosis , with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control[1]. TK216 has IC50s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line[1]. TK216 inhibits EWS-FLI1 (Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 fusion protein) protein interactions, leading to a decrease in transcription and proliferation[1]. |
In vivo | In the TMD-8 xenograft model, TK216 (po; 100 mg/kg; twice daily for 13 days) results in tumor growth inhibition [1]. |
Molecular Weight | 376.23 |
Formula | C19H15Cl2NO3 |
Cas No. | 1903783-48-1 |
Smiles | OC1(CC(=O)c2ccc(cc2)C2CC2)C(=O)Nc2c1c(Cl)ccc2Cl |
Relative Density. | 1.473 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 249 mg/mL (661.83 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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