| Identification | Back Directory | [Name]
5-(3-chlorophenylamino)-N-(2-hydroxyethyl)benzo[c][2,6]naphthyridine-8-carboxamide | [CAS]
2641079-92-5 | [Synonyms]
CK2 inhibitor 2,CK-2 inhibitor 2
5-(3-chlorophenylamino)-N-(2-hydroxyethyl)benzo[c][2,6]naphthyridine-8-carboxamide
Benzo[c]-2,6-naphthyridine-8-carboxamide, 5-[(3-chlorophenyl)amino]-N-(2-hydroxyethyl)- | [Molecular Formula]
C21H17ClN4O2 | [MDL Number]
MFCD34368514 | [MOL File]
2641079-92-5.mol | [Molecular Weight]
392.84 |
| Chemical Properties | Back Directory | [Boiling point ]
691.7±55.0 °C(Predicted) | [density ]
1.420±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.80±0.46(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity[1]. | [in vivo]
CK2 inhibitor 2 (60-90 mg/kg; p.o. twice a day for 4 weeks) obviously inhibits the tumor growth dose-dependently with a maximum inhibitory rate of 69% at a dose of 90 mg/kg[1].
CK2 inhibitor 2 (25 mg/kg; a single p.o.) exhibits Cmax (7017.8 ng/mL), elimination half-life (t1/2=6.67 h), and CL (0.60 L/h/kg) in SD rats[1]. | Animal Model: | Male BALB/c athymic nude mice (5 weeks old; 16-18 g) were injected HCT-116 cells[1] | | Dosage: | 60, 90 mg/kg | | Administration: | P.o. twice a day for 4 weeks | | Result: | Inhibited the tumor growth in a dose-dependent manner.
No conspicuous change in body weight. |
| Animal Model: | Sprague-Dawley (SD) rats[1] | | Dosage: | 25 mg/kg (Pharmacokinetic Analysis) | | Administration: | A single p.o. | | Result: | Cmax=7017.8 ng/mL, t1/2=6.67 h, CL=0.60 L/h/kg. |
| [IC 50]
CK2: 0.66 nM (IC50) | [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. DOI:10.1021/acs.jmedchem.1c00131 |
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