| Identification | Back Directory | [Name]
(3Z)-1,3-Dihydro-5-hydroxy-4,6-dimethyl-3-(2-quinolinylmethylene)-2H-pyrrolo[2,3-b]pyridin-2-one | [CAS]
2097497-16-8 | [Synonyms]
(3Z)-1,3-Dihydro-5-hydroxy-4,6-dimethyl-3-(2-quinolinylmethylene)-2H-pyrrolo[2,3-b]pyridin-2-one | [Molecular Formula]
C19H15N3O2 | [MOL File]
2097497-16-8.mol | [Molecular Weight]
317.34 |
| Chemical Properties | Back Directory | [Boiling point ]
667.8±55.0 °C(Predicted) | [density ]
1.377±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [pka]
10.22±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models[1]. | [in vivo]
Anticancer agent 109 (3 mg/kg, intraperitoneal injection, A549 tumor model for 31 days, PANC-1 tumor model for 85 days, six times a week) reduced tumor size and weight significantly in xenograft models of nude mice[1]. | Animal Model: | A549 or PANC-1 xenografted in BALB/c-nu mice[1]. | | Dosage: | 1 mg/kg; 3 mg/kg | | Administration: | Intraperitoneal injection (i.p.) 6 times a week | | Result: | Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models.
Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models.
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| [IC 50]
Axl | [References]
[1] Bae D, et al. Antitumor effect of 3-(quinolin-2-ylmethylene)-4,6-dimethyl-5-hydroxy-7-azaoxindole down-regulating the Gas6-Axl axis. Eur J Med Chem. 2023 May 5;251:115274. DOI:10.1016/j.ejmech.2023.115274 |
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