| Identification | Back Directory | [Name]
1-Naphthalenecarboxamide, N-(2-aminophenyl)-6-[(7-methoxy-4-quinolinyl)oxy]- | [CAS]
1256349-48-0 | [Synonyms]
Chiauranib
ibcasertib
Chiauranib (CS2164)
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 | [Molecular Formula]
C27H21N3O3 | [MDL Number]
MFCD34179475 | [MOL File]
1256349-48-0.mol | [Molecular Weight]
435.47 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
12.77±0.70(Predicted) | [color ]
White to light brown |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
Bide Pharmatech Ltd.
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| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
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