Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
ROCK2 5.7 nM (IC50) ROCK1 923 nM (IC50)
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ln Vitro |
THK01 (1.25-10 μM; 48 h) dose-dependently suppresses MDA-MB-231 cells' capacity for migration and invasion [1]. Using the STAT signaling pathway, THK01 (5 μM; 24 h; MDA-MB-231 cells) prevents breast cancer metastasis [1]. In a dose-dependent manner, THK01 (1.25-10 μM; 24 h; MDA-MB-231 cells) modestly increases the level of STAT3S727 while downregulating the phosphorylation of STAT3Y705 [1].
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ln Vivo |
THK01 (15 mg/kg; iv; female BALB/c nude mice) prevents the in vivo spread of breast cancer cells [1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Down-regulated the phosphorylation levels (p-STAT) of STAT1, STAT2, and STAT3, up-regulated of p-STAT5A and STAT6. Western Blot Analysis[1] Cell Types: MDA-MB-231 cells Tested Concentrations: 1.25, 2.5, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: decreased the level of p-STAT3Y705 and increased the expression of p-STAT3S727 in MDA-MB-231 cells. |
Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice with MDAMB-231-Luc-mcherry xenografts (6 weeks old, weight about 20 g)[1]
Doses: 15 mg/kg Route of Administration: intravenous (iv)injection; one time/day for 43 days Experimental Results: diminished the pulmonary metastasis of MDA-MB-231 in vivo with negligible toxicity. |
References |
[1]. Wang J, et, al. Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis. Eur J Med Chem. 2023 Mar 15;250:115181.
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Molecular Formula |
C20H13N3O2
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Molecular Weight |
327.34
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CAS # |
2226941-26-8
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SMILES |
O=C1NCC2=C3C4=CC=CC=C4NC3=C3NC4=CC=C(C=C4C3=C21)O
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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)
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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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0549 mL | 15.2746 mL | 30.5493 mL | |
5 mM | 0.6110 mL | 3.0549 mL | 6.1099 mL | |
10 mM | 0.3055 mL | 1.5275 mL | 3.0549 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.