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编 号:F528166
分子式:C23H24N4O
分子量:372.46
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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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(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer.

体内研究:
(E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth.?(E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners.Animal Model:Male BALB/c mice with HCT-116 colon cancer cells xenografts
Dosage:50 and 75 mg/kg
Administration:Oral gavage; 50 and 75 mg/kg once daily for 3 weeks
Result:Significantly inhibited the growth of tumors with a mean TGI of 82%.
Animal Model:Male BALB/c mice with lymphoma Ramos cells xenografts
Dosage:15 and 75 mg/kg
Administration:Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.)
Result:Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.

体外研究:
(E/Z)-Zotiraciclib (0-10 μM) shows potent inhibition to CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively.?(E/Z)-Zotiraciclib (0-10 μM; 48 h) inhibits proliferation of cancer cells.?(E/Z)-Zotiraciclib (8-1000 nM; 24 h) potently inhibits the CDK2 biomarker pRb in HCT-116 cells and potently againsts pRb in MV4-11 cells with an IC50 value of 0.13 μM.
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