1903783-48-1
1903783-48-1 structure
- Name: TK216
- Chemical Name: TK216
- CAS Number: 1903783-48-1
- Molecular Formula: C19H15Cl2NO3
- Molecular Weight: 376.23
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2019-12-07 18:18:54
- Modify Date: 2024-01-08 14:21:25
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TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions, leading to a decrease in transcription and proliferation. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 is active in oncogenesis and inhibits apoptosis[1].
| Name | TK216 |
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| Description | TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions, leading to a decrease in transcription and proliferation. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 is active in oncogenesis and inhibits apoptosis[1]. |
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| Related Catalog | |
| Target |
EWS-FLI1 protein[1] |
| In Vitro | TK-216 (500 nM; for 24-72 hours) induces apoptosis in DLBCL cell lines[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]. TK216 (0.1, 0.3, 1 μM) induces apoptosis in DLBCL cell lines, with the amount of cleaved-Caspase 3 normalized to b-actin and presented as fold over control[1]. TK-216 has IC50s of 0.363 μM and 0.152 μM for HL-60 AML cell line and TMD-8 DLBCL cell line[1]. Apoptosis Analysis[1] Cell Line: DLBCL cell lines Concentration: 500 nM Incubation Time: For 24, 48 or 72 hours Result: Induced apoptosis in DLBCL cell lines. |
| In Vivo | TK-216 (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. |
| References |
[1]. Brian Lannutti, et al. Uses of indolinone compounds. US10159660B2. |
| Molecular Formula | C19H15Cl2NO3 |
|---|---|
| Molecular Weight | 376.23 |
| Hazard Codes | Xn |
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