Description
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.
Product information
Molecular Weight: 392.84
Formula: C21H17ClN4O2
Chemical Name: 5-((3-chlorophenyl)amino)-N-(2-hydroxyethyl)benzo[c][2, 6]naphthyridine-8-carboxamide
Smiles: OCCNC(=O)C1=CC2=NC(NC3C=CC=C(Cl)C=3)=C3C=CN=CC3=C2C=C1
InChiKey: FPWXVWZFQXQWTH-UHFFFAOYSA-N
InChi: InChI=1S/C21H17ClN4O2/c22-14-2-1-3-15(11-14)25-20-17-6-7-23-12-18(17)16-5-4-13(10-19(16)26-20)21(28)24-8-9-27/h1-7,10-12,27H,8-9H2,(H,24,28)(H,25,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (127.28 mM; ultrasonic and warming and heat to 60°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CK2 inhibitor 2 (compound 1c) exhibits potent antiproliferative activities against PC-3, HCT-116, MCF-7, HT-29, T24 and LO2 cells, with IC50s of 4.53 μM, 3.07 μM, 7.50 μM, 5.18 μM, 6.10 μM, and 96.68 μM, respectively. CK2 inhibitor 2 (5-20 μM; 24 h) induces apoptosis of HCT-116 cells in a dose-dependent manner. CK2 inhibitor 2 dose-dependently suppresses the expression of p-Akt1S129 and p-Cdc37S13 in HCT-116 cells. CK2 inhibitor 2 (1-500 nM) dose-dependently inhibits exogenous ALDH1A1 enzyme activity, with an IC50 of 0.10 μM. CK2 inhibitor 2 (5-20 μM; 24 h) inhibits the transcription and protein expression of ALDH1A1 in HCT-116 cells.
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. 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.
Products are for research use only. Not for human use.
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