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TK216

Catalog No. T13166 CAS 1903783-48-1

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.

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TK216, CAS 1903783-48-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 313.00
50 mg	In stock	$ 538.00
100 mg	In stock	$ 778.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.45%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 249 mg/mL(661.83 mM)

References and Literature

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. 2. Brian Lannutti, et al. Uses of indolinone compounds. US10159660B2.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library PPI Inhibitor Library Cell Cycle Compound Library Pediatric Drug Library Clinical Compound Library Hematonosis Compound Library

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Related compounds with same targets

Nelarabine DMT-dG(ib) Phosphoramidite Nolatrexed AP-1/NF-κB activation inhibitor 1 Anticancer agent 73 Temozolomide Deoxycytidine triphosphate trisodium salt Sempervirine

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TK216 1903783-48-1 Cell Cycle/Checkpoint DNA Damage/DNA Repair Others DNA/RNA Synthesis Inhibitor EWS-FLI1 TK-216 transcription RNA proliferation EST inhibit sarcoma anticancer leukemia Ewing virus E26 Friend TK 216 inhibitor

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