Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 1.40 nM (TNK1)[1]
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ln Vitro |
Treatment with TP-5801 (10 pM-10 μM; 72 h) TFA reduces the development of Ba/F3 cells stimulated by TNK1, BCR-ABL, and IL-3 [1]. TNK1-dependent L540 cell proliferation is inhibited by TP-5801 (1 nM-10 μM; 10 d) TFA [1].
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ln Vivo |
TP-5801 (10 mg/kg; oral gavage, once) In a mouse tumor survival model, TFA is beneficial [1]. TP-5801 (oral gavage, once day, 50 mg/kg; 7 days) TFA can stop the growth of localized tumors [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Ba/F3 cells Tested Concentrations: 10 pM-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against WT TNK1 and AAA mutant cells, respectively. Inhibited BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively. Cell Viability Assay[1] Cell Types: L540 cells Tested Concentrations: 1, 10, 100, and 1000 nM Incubation Duration: 10 days Experimental Results: Inhibited TNK1-dependent L540 cell growth at low nM level. |
Animal Protocol |
Animal/Disease Models: Female NOD/SCID (severe combined immunodeficient) mouse injected with Ba/F3 luciferase cells expressing TNK1 AAA[1]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 10 mg/kg; once Experimental Results: demonstrated no signs of toxicity and Dramatically prolonged lifespan. Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse implanted subcutaneously (sc) with Ba/F3 luciferase cells expressing TNK1 AAA or BCR-ABL[1] Doses: 50 mg/kg Route of Administration: po (oral gavage); 50 mg/kg; one time/day; 7 days Experimental Results: decreased phospho -STAT3 in TNK1-driven xenografts at 2 hrs (hours) post-treatment, and tumor burden in mice xenografted. |
References |
[1]. Tsz-Yin Chan, et al. TNK1 is a ubiquitin-binding and 14-3-3-regulated kinase that can be targeted to block tumor growth. Nat Commun. 2021 Sep 9;12(1):5337.
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Molecular Formula |
C26H32BRF3N8O3
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Molecular Weight |
641.48
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Related CAS # |
TP-5801;2574474-81-8
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO :~100 mg/mL (~155.89 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5589 mL | 7.7945 mL | 15.5890 mL | |
5 mM | 0.3118 mL | 1.5589 mL | 3.1178 mL | |
10 mM | 0.1559 mL | 0.7794 mL | 1.5589 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.