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库存 :货期:电询
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规格 :电询
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CDK9-IN-28
MCE 国际站:CDK9-IN-28
产品活性:CDK9-IN-28 (化合物 10) 是一种有效的 CDK9 抑制剂。CDK9-IN-28 可作 PROTAC 靶蛋白配体,用于 PROTAC 合成。CDK9-IN-28 在实体瘤中显示出强大的抗增殖活性。
作用靶点:CDK
In Vitro: CDK9-IN-28 shows obvious CDK9 degradation in U-2932 cells and has obvious anti-proliferation activity in tumors.
In Vivo: CDK9-IN-28 (5 mg/kg, i.p., once a day for 15 days) inhibits the growth of tumors in MV4-11 Tumor Nude mice model.
CDK9-IN-28 (1mg/kg, i.v.,5 mg/kg, i.p., 15 days) exhibits an acceptable half-life (T1/2:4.66h) and moderate bioavailability (F = 43.1%) in ICR (CD-1) mice model。
药代动力学分析
T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (h*ng/mL) | CL_obs(mL/min/kg) | MRTINF_obs (h) | Vss_obs (mL/kg) | F (%) | |
i.p. 5 mg/kg | 4.66 | 0.25 | 88.4 | 156 | / | 4.17 | / | 43.1 |
i.v. 1 mg/kg | 1.97 | / | / | 72.3 | 229 | 0.79 | 10480 | / |
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