Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Targets |
CDK8 51.9 nM (IC50)
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ln Vitro |
In HCT-116 cells, CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 µM; 12 h) dose-dependently decreases the expression of p-STAT1 S727 and p-STAT5 S726[1]. Apoptosis is induced by CDK8-IN -13 (0, 1, 5, 10 µM; 48 h) in a dose-dependent manner [1].
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ln Vivo |
In mice, CDK8-IN-13 (40, 80 mg/kg; oral; for 15 days) dose-dependently suppresses the growth of tumors [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: molm-13, HL-60, MV4-11, MGC-803, MDA-MB-231, A375, A549 cells Tested Concentrations: 0-50 µM Incubation Duration: Experimental Results: demonstrated antiproliferative activity with GC50s of 1.57, 1.00, 4.61, >50, >50, >50, >50 µM, respectively. Western Blot Analysis[1] Cell Types: HCT-116 cells Tested Concentrations: 1, 2.5, 5, 10 µM Incubation Duration: 12 h Experimental Results: diminished the expression of p-STAT1 S727 and p-STAT5 S726, and suppressed the phosphorylation of STAT1 S727 induced by IFN-γ (10 ng/mL) in a dose-dependent manner. Apoptosis Analysis[1] Cell Types: HL-60 cells Tested Concentrations: 0, 1, 5, 10 µM Incubation Duration: 48 h Experimental Results: Induced approximately 7% and 36% apoptotic at concentrations of 5 and 10 μM, respectively. |
Animal Protocol |
Animal/Disease Models: 6weeks old balb/c (Bagg ALBino) mouse: (C1498 cells)[1]
Doses: 40, 80 mg/kg Route of Administration: Po; for 15 days Experimental Results: diminished the tumor growth with no significant weight loss, the expression of Ki67 diminished in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated. |
References |
[1]. Zhang XX, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia. Eur J Med Chem. 2023 May 5;251:115214.
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Molecular Formula |
C14H11N3O
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Molecular Weight |
237.26
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CAS # |
918523-75-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(N)(=O)C1=CC=CC(C2=CN=C3NC=CC3=C2)=C1
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HS Tariff Code |
2934.99.9001
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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 Vitro) |
DMSO : 125 mg/mL (526.85 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 | 4.2148 mL | 21.0739 mL | 42.1479 mL | |
5 mM | 0.8430 mL | 4.2148 mL | 8.4296 mL | |
10 mM | 0.4215 mL | 2.1074 mL | 4.2148 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.