| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
CK2 0.66 nM (IC50)
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| ln Vitro |
CK2 inhibitor 2 (compound 1c) has strong antiproliferative properties against PC-3, HCT-116, MCF-7, HT-29, T24, and LO2 cells. Its IC50 values are 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, in that order[1]. HCT-116 cells experience dose-dependent apoptosis when exposed to CK2 inhibitor 2 (5–20 μM; 24 h). In HCT-116 cells, CK2 inhibitor 2 dose-dependently decreases the expression of p-Akt1S129 and p-Cdc37S13[1]. The exogenous ALDH1A1 enzyme activity is dose-dependently inhibited by CK2 inhibitor 2 (1-500 nM), with an IC50 of 0.10 μM[1]. In HCT-116 cells, CK2 inhibitor 2 (5-20 μM; 24 h) suppresses ALDH1A1 transcription and protein expression[1].
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| ln Vivo |
It is clear that CK2 inhibitor 2 (60–90 mg/kg; po twice day for 4 weeks) inhibits tumor growth in a dose-dependent manner, reaching a maximum inhibitory rate of 69% at 90 mg/kg[1]. The Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) of CK2 inhibitor 2 (25 mg/kg; single po) in SD rats[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: HCT-116 cells Tested Concentrations: 5, 10, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: The apoptotic ratio reached about 55% at the concentration of 20 μM. Western Blot Analysis[1] Cell Types: HCT-116 cells Tested Concentrations: 5, 10, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the expression of p-Akt1S129 and p-Cdc37S13 in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c athymic nude mice (5 weeks old; 16-18 g) were injected HCT-116 cells[1]
Doses: 60, 90 mg/kg Route of Administration: Po twice a day for 4 weeks Experimental Results: Inhibited the tumor growth in a dose-dependent manner. No conspicuous change in body weight. Animal/Disease Models: SD (Sprague-Dawley) rats[1] Doses: 25 mg/ kg (pharmacokinetic/PK Analysis) Route of Administration: A single po Experimental Results: Cmax=7017.8 ng/mL, t1/2=6.67 h, CL=0.60 L/h/kg. |
| References |
[1]. Wang Y, et, al. Discovery of 5-(3-Chlorophenylamino)benzo[ c][2,6]naphthyridine Derivatives as Highly Selective CK2 Inhibitors with Potent Cancer Cell Stemness Inhibition. J Med Chem. 2021 Apr 22;64(8):5082-5098.
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| Molecular Formula |
C21H17CLN4O2
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|---|---|
| Molecular Weight |
392.84
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| CAS # |
2641079-92-5
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| SMILES |
C1(NC2=CC=CC(Cl)=C2)C2=C(C=NC=C2)C2=CC=C(C(NCCO)=O)C=C2N=1
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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 : 50 mg/mL (127.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.29 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5456 mL | 12.7278 mL | 25.4557 mL | |
| 5 mM | 0.5091 mL | 2.5456 mL | 5.0911 mL | |
| 10 mM | 0.2546 mL | 1.2728 mL | 2.5456 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.
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