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编 号：F756189
分子式：C19H22N8O2
分子量：394.43
分子式：C19H22N8O2
分子量：394.43
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CAS No: 2823369-81-7
产品详情
生物活性：
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin.
体内研究：
DNA-PK-IN-8 (100 mg/kg; PO; QD for 16 days) significantly suppresses HL-60 tumor growth when co-administrating with Doxorubicin.DNA-PK-IN-8 (5 mg/kg; PO; single dosage) exhibits reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.Pharmacokinetic Parameters of DNA-PK-IN-8 in Sprague-Dawley rats. PO (5 mg/kg)
Tmax (h)0.42 ± 0.11
t1/2 (h)1.59 ± 0.26
Cmax (ng/mL)810 ± 122.32
AUC0-∞ (ng/mL·h)3598.7 ± 769.81
MRT0-∞ (h)2.29 ± 0.18
Animal Model:HL-60 tumor-bearing nude mice model
Dosage:100 mg/kg
Administration:PO; QD for 16 days
Result:Led to significant tumor-suppressing effects with TGI values of 52.4% and 62.4% for tumor weight and tumor volume, respectively, when co-administrated with Doxorubicin.
Animal Model:Sprague-Dawley rats
Dosage:5 mg/kg
Administration:PO; single dosage (Pharmacokinetic Analysis)
Result:Exhibited reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.
体外研究：
DNA-PK-IN-8 (compound DK1) decreases the expression levels of γH2A.X in a concentration-dependent manner in HCT-116 cells.
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin.
体内研究：
DNA-PK-IN-8 (100 mg/kg; PO; QD for 16 days) significantly suppresses HL-60 tumor growth when co-administrating with Doxorubicin.DNA-PK-IN-8 (5 mg/kg; PO; single dosage) exhibits reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.Pharmacokinetic Parameters of DNA-PK-IN-8 in Sprague-Dawley rats. PO (5 mg/kg)
Tmax (h)0.42 ± 0.11
t1/2 (h)1.59 ± 0.26
Cmax (ng/mL)810 ± 122.32
AUC0-∞ (ng/mL·h)3598.7 ± 769.81
MRT0-∞ (h)2.29 ± 0.18
Animal Model:HL-60 tumor-bearing nude mice model
Dosage:100 mg/kg
Administration:PO; QD for 16 days
Result:Led to significant tumor-suppressing effects with TGI values of 52.4% and 62.4% for tumor weight and tumor volume, respectively, when co-administrated with Doxorubicin.
Animal Model:Sprague-Dawley rats
Dosage:5 mg/kg
Administration:PO; single dosage (Pharmacokinetic Analysis)
Result:Exhibited reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.
体外研究：
DNA-PK-IN-8 (compound DK1) decreases the expression levels of γH2A.X in a concentration-dependent manner in HCT-116 cells.
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