Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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Targets |
CLK1 5 nM (IC50) CLK2 42 nM (IC50) CLK4 108 nM (IC50) DYRK1A 1521 nM (IC50)
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ln Vitro |
CLK1-IN-3 (compound 10ad) has the capacity to inhibit both Clk1 and Clk2, which gives it anti-tumor potential [1]. In a dose-dependent manner, CLK1-IN-3 (10 μM-1000 μM) may bind to Clk1 protein and efficiently block its degradation [1]. In HeLa, BNLCL.2, and HCT 116 cells, CLK1-IN-3 (0–10 μM, 24 h) initiates autophagy [1]. The autolysosomal marker SQSTM1/p62 is degraded more readily when CLK1-IN-3 is present [1].
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ln Vivo |
In the acetaminophen (HY-66005, APAP)-induced ALI model, CLK1-IN-3 (compound 10ad) (0-40 mg/kg, intraperitoneal injection, once) can significantly inhibit ALI without obvious hepatocyte death[1]. With an acceptable pharmacokinetic profile and a relatively long half-life of 5.29 hours, CLK1-IN-3 (10 mg/kg; IV, PO, IP, once) has an oral bioavailability of 19.5%[1].
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Cell Assay |
Western Blot Analysis[1]
Cell Types: Hela cells, BNLCL.2 and HCT 116 cells Tested Concentrations: 0.2, 1, 5, and 10 μM Incubation Duration: 24 h Experimental Results: Elevated the expression level of LC3II protein (a marker of autophagosomes) as well as the ratio of LC3II to LC3I (a sensitive index of autophagy) in a dose-dependent and time-dependent manner. |
Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice(8 weeks, injected acetaminophen (HY-66005) (500 mg/kg, ip))[1]
Doses: 10, 20, and 40 mg/kg Route of Administration: IP, once Experimental Results: diminished serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels Dramatically in dose-dependent. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse: (aged 8 weeks)[1] Doses: 10 mg/kg Route of Administration: IV, PO, IP, once (pharmacokinetic/PK Analysis) Experimental Results: pharmacokinetic/PK Parameters of CLK1-IN-3 in male balb/c (Bagg ALBino) mouse:[1]. IV (10 mg/kg) PO ( 10 mg/kg) IP (10 mg/kg) Cmax (ng/mL) 13166.5±875.9 1457.4±177.3 4654.3±435.3 T1/2 (h) 2.96±1.2 5.29±2.1 3.27 ±1.1 AUC0-t (ng/mL* h) 9520.5±1011.3 1860.2±411.0 5010.4±987.2 CL (L/h/kg) 1.05±0.10 5.51±1.00 3.58±0.82 F (%) 19.5% |
References |
[1]. Yang T, et al. Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI). Eur J Med Chem. 2023 Mar 15;250:115168.
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Molecular Formula |
C24H23FN6O
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Molecular Weight |
430.48
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CAS # |
2922550-28-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3230 mL | 11.6149 mL | 23.2299 mL | |
5 mM | 0.4646 mL | 2.3230 mL | 4.6460 mL | |
10 mM | 0.2323 mL | 1.1615 mL | 2.3230 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.