| Identification | Back Directory | [Name]
CQ211 | [CAS]
2648986-65-4 | [Synonyms]
CQ211
4H-1,2,3-Triazolo[4,5-c]quinolin-4-one, 1,5-dihydro-8-(6-methoxy-3-pyridinyl)-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]- | [Molecular Formula]
C26H22F3N7O2 | [MOL File]
2648986-65-4.mol | [Molecular Weight]
521.49 |
| Chemical Properties | Back Directory | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
9.92±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
CQ211 is a potent and selective RIOK2 inhibitor with a Kd of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines[1]. | [Biological Activity]
CQ211 is a cell penetrantselective and highly potent RIOK2 (Right open reading frame kinase 2) inhibitor. CQ211 potently inhibits proliferation of multiple cancer cell lines including MKN-1 and HT-29 cells. It inhibits tumor progression in MKN-1 xenograft model after intraperitoneal administration. | [in vivo]
CQ211 (25 mg/kg; i.p; for 18 consecutive days; once daily) inhibits MKN-1 xenograft mouse model[1]. | Animal Model: | Female CB17-SCID mice (6-8 weeks of age) injected wtih MKN-1 cells[1] | | Dosage: | 25 mg/kg | | Administration: | Intraperitoneal administration; for 18 consecutive days; once daily | | Result: | Inhibited the tumor progression with tumor growth inhibition (TGI) of 30.9%. |
| [References]
[1] Ouyang Y, et al. Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. J Med Chem. 2022 Jun 9;65(11):7833-7842. DOI:10.1021/acs.jmedchem.2c00271 |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|