| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| Targets |
ETS
|
|---|---|
| ln Vitro |
In DLBCL cell lines, TK216 (500 nM) induces apoptosis for a duration of 24-72 hours [1]. In the Ewing sarcoma A4573 cell line, TK216 (0.03, 0.06, 0.125, 0.25, 0.5 μM) inhibits growth in a dose-dependent manner [1]. DLBCL cell lines are exposed to TK216 (0.1, 0.3, and 1 μM) to induce apoptosis; the amount of cleaved caspase 3 is normalized to b-actin and displayed as fold over control [1]. TK216's half maximal inhibitory concentration (IC50) for the HL-60 AML and TMD-8 DLBCL cell lines are 0.363 μM and 0.152 μM, respectively[1]. Reduced transcription and proliferation are the results of TK216's inhibition of the EWS-FLI1 (Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 fusion protein) protein interaction [1].
|
| ln Vivo |
In TMD-8 xenograft models, TK216 (100 mg/kg orally; twice daily for 13 days) reduces the formation of tumors [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: DLBCL cell lines Tested Concentrations: 500 nM Incubation Duration: For 24, 48 or 72 hrs (hours) Experimental Results: Induced apoptosis in DLBCL cell lines. |
| Animal Protocol |
Animal/Disease Models: NOD-SCID (severe combined immunodeficient) mouse subcutaneously (sc) inoculated with TMD8 cells[1]
Doses: 100 mg/kg Route of Administration: PO; twice (two times) daily for 13 days Experimental Results: Resulted in tumor growth inhibition. |
| 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.
[2]. Brian Lannutti, et al. Uses of indolinone compounds. US10159660B2. |
| Molecular Formula |
C19H15CL2NO3
|
|---|---|
| Molecular Weight |
376.23
|
| Exact Mass |
375.04
|
| Elemental Analysis |
C, 60.66; H, 4.02; Cl, 18.84; N, 3.72; O, 12.76
|
| CAS # |
1903783-48-1
|
| Related CAS # |
1903783-48-1 (racemic); 1903783-78-7 (rotation -)
|
| Appearance |
Solid powder
|
| SMILES |
C1CC1C2=CC=C(C=C2)C(=O)CC3(C4=C(C=CC(=C4NC3=O)Cl)Cl)O
|
| InChi Key |
ZWHNLSHDLKIXOG-UHFFFAOYSA-N
|
| InChi Code |
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)
|
| Chemical Name |
4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one
|
| Synonyms |
TK-216; TK216; TK 216
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 250 mg/mL (~664.5 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6579 mL | 13.2897 mL | 26.5795 mL | |
| 5 mM | 0.5316 mL | 2.6579 mL | 5.3159 mL | |
| 10 mM | 0.2658 mL | 1.3290 mL | 2.6579 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05046314 | Not yet recruiting | Biological: TK216+Vincristin | Sarcoma, Ewing | Shanghai Pharmaceuticals Holding Co., Ltd |
October 28, 2024 | Phase 2 |
| NCT02657005 | Terminated | Drug: TK216 | Sarcoma, Ewing | Oncternal Therapeutics, Inc | August 2016 | Phase 1 Phase 2 |
| NCT03752138 | Withdrawn | Drug: Group 1: TK216 Drug: Group 2: TK216 |
Recurrent Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia |
M.D. Anderson Cancer Center | March 31, 2019 | Phase 1 |
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
