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编 号:F197794
分子式:C17H10F6N6O
分子量:428.29
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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:
Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines.

体内研究:
KPT-8602 (15 mg/kg;口服填喂法;每日给药;共 12 天) 显示出有效的抗淋巴细胞白血病活性。Animal Model:Female BALB/c mice (model with the JAK3 (M511I) mutation)
Dosage:15 mg/kg
Administration:Oral gavage; daily for 12 days
Result:Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12.

体外研究:
KPT-8602 (2-6 nM;EC50s范围在25 ~ 145 nM KPT-8602 (1 nM;。”
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