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编 号:F532771
分子式:C19H16ClNO4
分子量:357.79
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.

体内研究:
A-803467 (35 mg/kg; p.o.) shows no noticeable toxicity in the male NCR nude mice.A-803467 in combination with topotecan, significantly decreases the tumor growth in mice implanted with ABCG2 overexpressing H460/MX20 cells. A-803467 effectively restores the sensitivity of tumors overexpressing ABCG2 transporter to topotecan without having any significant effect on tumors lacking ABCG2 expression.Animal Model:Nude mice
Dosage:35 mg/kg
Administration:P.o.
Result:Showed no noticeable toxicity in the male NCR nude mice.

体外研究:
A-803467 selectively and significantly reverses the ABCG2-mediated multidrug resistance. A-803467 (7.5 μM) significantly increases the cytotoxicity of mitoxantrone and topotecan in ABCG2-transfected cell lines. A-803467 (7.5 μM) significantly enhanced theintracellular [3H]-MX accumulation in ABCG2-transfected cells. A-803467 (7.5 μM; 0~120 minutes) significantly blocks the intracellular [3H]-MX efflux at different time periods from ABCG2-transfected cells. A-803467 stimulates the ATPase activity of ABCG2.
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