产品
编 号：F151960
分子式：C29H40FN5O2
分子量：509.66
分子式：C29H40FN5O2
分子量：509.66
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CAS No: 1403898-55-4
产品详情
生物活性：
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
体内研究：
XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner.XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg.Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice.dose (mg/kg)route Tmax (h) Cmax (μg/mL)CLp (mL/min/kg)Vss (L/kg)half life (h)AUC (μg·h/mL)F (%)
1IV40.96.43.00.41
5PO20.121.80.4522
30PO11.712.1
Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts
Dosage:7.5, 15, 30 mg/kg
Administration:PO; daily for 24 days
Result:Inhibited the tumor growth in dose-dependent manner.
Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts
Dosage:
Administration:1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result:Showed oral bioavailability (F=22%).
体外研究：
XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM.
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
体内研究：
XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner.XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg.Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice.dose (mg/kg)route Tmax (h) Cmax (μg/mL)CLp (mL/min/kg)Vss (L/kg)half life (h)AUC (μg·h/mL)F (%)
1IV40.96.43.00.41
5PO20.121.80.4522
30PO11.712.1
Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts
Dosage:7.5, 15, 30 mg/kg
Administration:PO; daily for 24 days
Result:Inhibited the tumor growth in dose-dependent manner.
Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts
Dosage:
Administration:1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result:Showed oral bioavailability (F=22%).
体外研究：
XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM.
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