产品
编 号：F755844
分子式：C24H21N7O2
分子量：439.47
分子式：C24H21N7O2
分子量：439.47
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CAS No: 2767560-51-8
产品详情
生物活性：
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
体内研究：
A2AAR/HDAC-IN-1 (compound 14c) (30 or 60 mg/kg, IP, twice daily for 9 days) shows potent anti-tumor effects in the mouse MC38 xenograft model.A2AAR/HDAC-IN-1 (90 mg/kg, bid; 150 mg/kg, qd; Oral gavage, for 15 days) shows weak tumor suppression.A2AAR/HDAC-IN-1 (5 mg/kg, IV; 20 mg/kg PO or IP; once) shows an overall favorable pharmacokinetic profile.Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)
Dosage:30 or 60 mg/kg
Administration:IP, twice daily for 9 days
Result:Significantly inhibited tumor growth at a dosage of 30 mg/kg (ip, bid), with a tumor growth inhibition (TGI) rate of 68%. At a dosage of 60 mg/kg, the TGI rate was further increased to 85%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)
Dosage:90 mg/kg, bid; 150 mg/kg, qd
Administration:Oral gavage, twice daily (90 mg/kg) or daily (150 mg/kg), for 15 days
Result:Showed only weak tumor suppression even at a dose of 90 mg/kg (po, bid), with inhibition rates of 44%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight)
Dosage:5 mg/kg (IV) and 20 mg/kg (PO, IP)
Administration:Orally, IP, or IV; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of A2AAR/HDAC-IN-1 in male ICR mice.PK Parameterspo (20 mg/kg) iv (5 mg/kg) ip (20 mg/kg)
Kel (h-1)0.390 ± 0.1871.820 ± 0.3000.844 ± 0.021
t1/2 (h)2.24 ± 1.160.389 ± 0.0700.83 ± 0.02
Tmax (h)0.333 ± 0.140.25 ± 0.00
Cmax (ng/mL)3417 ± 16394703 ± 7358411 ± 693
C0 (ng/mL)6498 ± 1285
AUC0-t (ng/mL·h)3602 ± 18072098 ± 14310022 ± 931
CL (mL/min/kg)39.3 ± 2.333.5 ± 3.1
体外研究：
A2AAR/HDAC-IN-1 (compound 14c) (0-100 μM, 72 h) shows anti-proliferative activities against colon cancer cell lines, CT26 and MC38.A2AAR/HDAC-IN-1 (0-5 μM, 24 h) increases histone acetylation.A2AAR/HDAC-IN-1 shows moderate selectivity against A1AR (3-fold) and no significant binding for A2BAR and A3AR.
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
体内研究：
A2AAR/HDAC-IN-1 (compound 14c) (30 or 60 mg/kg, IP, twice daily for 9 days) shows potent anti-tumor effects in the mouse MC38 xenograft model.A2AAR/HDAC-IN-1 (90 mg/kg, bid; 150 mg/kg, qd; Oral gavage, for 15 days) shows weak tumor suppression.A2AAR/HDAC-IN-1 (5 mg/kg, IV; 20 mg/kg PO or IP; once) shows an overall favorable pharmacokinetic profile.Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)
Dosage:30 or 60 mg/kg
Administration:IP, twice daily for 9 days
Result:Significantly inhibited tumor growth at a dosage of 30 mg/kg (ip, bid), with a tumor growth inhibition (TGI) rate of 68%. At a dosage of 60 mg/kg, the TGI rate was further increased to 85%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)
Dosage:90 mg/kg, bid; 150 mg/kg, qd
Administration:Oral gavage, twice daily (90 mg/kg) or daily (150 mg/kg), for 15 days
Result:Showed only weak tumor suppression even at a dose of 90 mg/kg (po, bid), with inhibition rates of 44%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight)
Dosage:5 mg/kg (IV) and 20 mg/kg (PO, IP)
Administration:Orally, IP, or IV; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of A2AAR/HDAC-IN-1 in male ICR mice.PK Parameterspo (20 mg/kg) iv (5 mg/kg) ip (20 mg/kg)
Kel (h-1)0.390 ± 0.1871.820 ± 0.3000.844 ± 0.021
t1/2 (h)2.24 ± 1.160.389 ± 0.0700.83 ± 0.02
Tmax (h)0.333 ± 0.140.25 ± 0.00
Cmax (ng/mL)3417 ± 16394703 ± 7358411 ± 693
C0 (ng/mL)6498 ± 1285
AUC0-t (ng/mL·h)3602 ± 18072098 ± 14310022 ± 931
CL (mL/min/kg)39.3 ± 2.333.5 ± 3.1
体外研究：
A2AAR/HDAC-IN-1 (compound 14c) (0-100 μM, 72 h) shows anti-proliferative activities against colon cancer cell lines, CT26 and MC38.A2AAR/HDAC-IN-1 (0-5 μM, 24 h) increases histone acetylation.A2AAR/HDAC-IN-1 shows moderate selectivity against A1AR (3-fold) and no significant binding for A2BAR and A3AR.
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