1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-
- Product Name
- 1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-
- CAS No.
- 1256349-48-0
- Chemical Name
- 1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-
- Synonyms
- Chiauranib;ibcasertib;Chiauranib (CS2164);Chiauranib/1256349-48-0;Chiauranib, 10 mM in DMSO;N-(2-Aminophenyl)-6-((7-methoxyquinolin-4-yl)oxy)-1-naphthamide;N-(2-Aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-1-naphthalenecarboxamide;1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]-;CSF-1R,VEGFR2,CSF1R,Vascular endothelial growth factor receptor,VEGFR3,anti-angiogenesis,CD117,Aurora Kinase,c-Kit,CS-2164,CSF-1 receptor,Chiauranib,colony stimulating factor 1 receptor,PDGFRα,PDGFR,Aurora-B,anticancer,inhibit,SCFR,Inhibitor,VEGFR,Platelet-derived growth factor receptor,CS 2164,VEGFR1,c-Fms
- CBNumber
- CB98119659
- Molecular Formula
- C27H21N3O3
- Formula Weight
- 435.47
- MOL File
- 1256349-48-0.mol
1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]- Property
- Boiling point:
- 604.6±50.0 °C(Predicted)
- Density
- 1.333±0.06 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO : 62.5 mg/mL (143.52 mM; Need ultrasonic)
- pka
- 12.77±0.70(Predicted)
- form
- Solid
- color
- White to light brown
1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]- Chemical Properties,Usage,Production
Uses
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects[1].
in vivo
Chiauranib (CS2164; 0.5-40 mg/kg; oral administration; once daily; for 33 days or 43 days) treatment induces remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models. Chiauranib exhibits broad and potent in vivo anti-tumor activities[1].
| Animal Model: | Female BALB/c athymic (nu+/nu+) mice (6-week old) bearing HCT-8, SMMC-7721, MGC‐803 or A549 cells[1] |
| Dosage: | 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg |
| Administration: | Oral administration; once daily; for 33 days or 43 days |
| Result: | Induced remarkable regression or complete inhibition of tumor growth in several human tumor xenograft models. |
IC 50
Flt-1: 8 nM (IC50); KDR: 7 nM (IC50); Flt-4: 9 nM (IC50); PDGFRα: 1 nM (IC50); c-Kit: 4 nM (IC50); Aurora B: 9 nM (IC50); PDGFRβ: 93 nM (IC50); CSF-1R: 7 nM (IC50)
References
[1] You Zhou, et al. CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci. 2017 Mar;108(3):469-477. DOI:10.1111/cas.13141
1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]- Preparation Products And Raw materials
Raw materials
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