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编 号：F756787
分子式：C35H32ClF3N3O10P
分子量：778.06
分子式：C35H32ClF3N3O10P
分子量：778.06
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CAS No: 2912285-84-6
产品详情
生物活性：
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 μM). CREB-IN-1 TFA inhibits breast cancer cell growth.
体内研究：
CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%.Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice .routedose(mg/kg) t1/2(h) Tmax(h)Cmax(ng/mL)AUC0-t(ng·hr/mL)AUC0-∞((ng·hr/mL)bioavailability (F%)
IP104.21.0156892910144
PO205.52.007346847938
Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO.Animal Model:Female C57BL/6 mice
Dosage:5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H2O at 40 mg/mL and further dilutions were made using ddI H2O)
Administration:Showed much improve oral bioavailability at 38%.
Result:Showed much improve oral bioavailability at 38%.
体外研究：
CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 μM; 24 hours) inhibits CREB-mediated gene transcription with an IC50 of 0.18 μM.CREB-IN-1 TFA (100 μM; 3 days) shows potent activities in MDA-MB-231 (GI50=0.38 μM) and MDA-MB-468 (GI50=0.021 μM) cells.
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 μM). CREB-IN-1 TFA inhibits breast cancer cell growth.
体内研究：
CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%.Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice .routedose(mg/kg) t1/2(h) Tmax(h)Cmax(ng/mL)AUC0-t(ng·hr/mL)AUC0-∞((ng·hr/mL)bioavailability (F%)
IP104.21.0156892910144
PO205.52.007346847938
Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO.Animal Model:Female C57BL/6 mice
Dosage:5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H2O at 40 mg/mL and further dilutions were made using ddI H2O)
Administration:Showed much improve oral bioavailability at 38%.
Result:Showed much improve oral bioavailability at 38%.
体外研究：
CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 μM; 24 hours) inhibits CREB-mediated gene transcription with an IC50 of 0.18 μM.CREB-IN-1 TFA (100 μM; 3 days) shows potent activities in MDA-MB-231 (GI50=0.38 μM) and MDA-MB-468 (GI50=0.021 μM) cells.
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