产品
编 号：F756133
分子式：C43H53N13O8
分子量：879.96
分子式：C43H53N13O8
分子量：879.96
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2816929-47-0
产品详情
生物活性：
STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
体内研究：
STING agonist-17 (compound 4a) (Intravenous injection; 0.015 mg/kg, 1.5 mg/kg; every other day; a week) has an inhibitory effect on tumor growth in CT26 cells-derived colon carcinoma female BALB/c mice.The pharmacokinetic parameters of Compound 4a in vivo.ParameterCompound 4a
T1/2 (h)10.54 ± 4.10
Vss (L/kg)>17.74 ± 5.29
CL (L/h/kg)2.12 ± 0.27
AUClast (μg?h/mL)4.20 ± 0.26
AUC∞ (μg?h/mL)>4.78 ± 0.59
Animal Model:Female BALB/c mice aged 6 weeks
Dosage:0.015 mg/kg, 1.5 mg/kg
Administration:Intravenous injection; every other day; a week
Result:Inhibited tumor growth in both doses and caused 57% inhibition at a concentration of 1.5 mg/kg on the 17th day without weight loss.
体外研究：
STING agonist-17 (compound 4a) inhibits the activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19 and CYP2D6) with IC50 values > 100 μM and for CYP3A4 with an IC50 = 4.2 μM.STING agonist-17 (compound 4a) (0-2 μM, 24 hours) induces IFN-β secretion with the EC50 of 2.0 nM.STING agonist-17 (compound 4a) (2 nM, 10 nM, 6 hours) can induce the expression of signal transduction factors.The pharmacokinetic parameters of Compound 4a in vitro.ParameterCompound 4a
CYP inhibition (IC50, μM)
1A2>100.0
2C9>100.0
2C19>100.0
2D6>100.0
3A44.2
Cardiotoxicity (IC50, μM)
hERG patch clamp assay>50.0
Liver microsomal phase I stability
mouse (%)38.7 ± 2.6
human (%)11.2 ± 2.7
Plasma stability
mouse (%)>99
human (%)>99
STING agonist-17 (compound 4a) is a potent STING agonist with an IC50 value of 0.062 nM. STING agonist-17 has anti-cancer activity for tumor immunization.
体内研究：
STING agonist-17 (compound 4a) (Intravenous injection; 0.015 mg/kg, 1.5 mg/kg; every other day; a week) has an inhibitory effect on tumor growth in CT26 cells-derived colon carcinoma female BALB/c mice.The pharmacokinetic parameters of Compound 4a in vivo.ParameterCompound 4a
T1/2 (h)10.54 ± 4.10
Vss (L/kg)>17.74 ± 5.29
CL (L/h/kg)2.12 ± 0.27
AUClast (μg?h/mL)4.20 ± 0.26
AUC∞ (μg?h/mL)>4.78 ± 0.59
Animal Model:Female BALB/c mice aged 6 weeks
Dosage:0.015 mg/kg, 1.5 mg/kg
Administration:Intravenous injection; every other day; a week
Result:Inhibited tumor growth in both doses and caused 57% inhibition at a concentration of 1.5 mg/kg on the 17th day without weight loss.
体外研究：
STING agonist-17 (compound 4a) inhibits the activity of four major CYP isozymes (CYP1A2, CYP2C9, CYP2C19 and CYP2D6) with IC50 values > 100 μM and for CYP3A4 with an IC50 = 4.2 μM.STING agonist-17 (compound 4a) (0-2 μM, 24 hours) induces IFN-β secretion with the EC50 of 2.0 nM.STING agonist-17 (compound 4a) (2 nM, 10 nM, 6 hours) can induce the expression of signal transduction factors.The pharmacokinetic parameters of Compound 4a in vitro.ParameterCompound 4a
CYP inhibition (IC50, μM)
1A2>100.0
2C9>100.0
2C19>100.0
2D6>100.0
3A44.2
Cardiotoxicity (IC50, μM)
hERG patch clamp assay>50.0
Liver microsomal phase I stability
mouse (%)38.7 ± 2.6
human (%)11.2 ± 2.7
Plasma stability
mouse (%)>99
human (%)>99
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