产品
编 号：F762562
分子式：C29H31N5O4S
分子量：545.65
分子式：C29H31N5O4S
分子量：545.65
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CAS No: 3012609-63-8
产品详情
生物活性：
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.
体内研究：
ATR-IN-20 (compound 48f) shows a favorable pharmacokinetic profile with a bioavailability of 30.0% in SD rats, acceptable plasma protein binding (PPB), high permeability, and low risk of drug-drug interactions.Mean values of pharmacokinetic parameters of ATR-IN-20 (compound 48f) after an i.v. at 1 mg/kg in Sprague-Dawley Rats.ParametersATR-IN-20 (compound 48f)
T1/2 (h)1.32
MRT0-inf (h)1.45
MRT0-t (h)1.36
AUC0-inf (ng·h·mL?1)1170
AUC0-t (ng·h·mL?1)1160
CL (mL·kg?1·min?1)14.2
Vdss (L·kg?1)1.24
体外研究：
ATR-IN-20 (compound 48f; 0.03-3 μM; 24 hours) significantly inhibits migrating in a concentration-dependent manner in LoVo cells.ATR-IN-20 (compound 48f) displays strong monotherapy efficacy in ATM kinase-deficient tumor cells LoVo, SW620, OVCAR-3 cell lines with IC50 values of 0.040 μM, 0.095 μM, 0.098 μM, respectively. ATR-IN-20 (compound 48f; 0.03-3 μM) decreases the colony-forming ability in a dose-dependent manner in LoVo cells.ATR-IN-20 (compound 48f) shows no significant inhibition against CYP1A2, CYP2C9, and CYP2D6. However, ATR-IN-20 exhibits a weak inhibitory potency against CYP2C19 and CYP3A4 with IC50 values of 1 μM.
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.
体内研究：
ATR-IN-20 (compound 48f) shows a favorable pharmacokinetic profile with a bioavailability of 30.0% in SD rats, acceptable plasma protein binding (PPB), high permeability, and low risk of drug-drug interactions.Mean values of pharmacokinetic parameters of ATR-IN-20 (compound 48f) after an i.v. at 1 mg/kg in Sprague-Dawley Rats.ParametersATR-IN-20 (compound 48f)
T1/2 (h)1.32
MRT0-inf (h)1.45
MRT0-t (h)1.36
AUC0-inf (ng·h·mL?1)1170
AUC0-t (ng·h·mL?1)1160
CL (mL·kg?1·min?1)14.2
Vdss (L·kg?1)1.24
体外研究：
ATR-IN-20 (compound 48f; 0.03-3 μM; 24 hours) significantly inhibits migrating in a concentration-dependent manner in LoVo cells.ATR-IN-20 (compound 48f) displays strong monotherapy efficacy in ATM kinase-deficient tumor cells LoVo, SW620, OVCAR-3 cell lines with IC50 values of 0.040 μM, 0.095 μM, 0.098 μM, respectively. ATR-IN-20 (compound 48f; 0.03-3 μM) decreases the colony-forming ability in a dose-dependent manner in LoVo cells.ATR-IN-20 (compound 48f) shows no significant inhibition against CYP1A2, CYP2C9, and CYP2D6. However, ATR-IN-20 exhibits a weak inhibitory potency against CYP2C19 and CYP3A4 with IC50 values of 1 μM.
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