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  3. CREB-IN-1 TFA

CREB-IN-1 TFA 

Cat. No.: HY-144318
Handling Instructions

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.

For research use only. We do not sell to patients.

CREB-IN-1 TFA Chemical Structure

CREB-IN-1 TFA Chemical Structure

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Description

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth[1].

IC50 & Target

IC50: 0.18 µM (CREB)[1]

In Vitro

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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HEK 293T cells
Concentration: 100 µM
Incubation Time: 24 hours
Result: Inhibited CREB-mediated gene transcription with an IC50 of 0.18 µM.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 100 µM
Incubation Time: 3 days
Result: Showed potent activities in MDA-MB-231 (GI50 =0.38 µM) and MDA-MB-468 (GI50 =0.021 µM) cells.
In Vivo

CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%[1].
Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice [1].

route dose(mg/kg) t1/2(h) Tmax(h) Cmax(ng/mL) AUC0-t(ng·hr/mL) AUC0-∞((ng·hr/mL) bioavailability (F%)
IP 10 4.2 1.0 156 892 910 144
PO 20 5.5 2.00 73 468 479 38

Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 mice[1]
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%.
Molecular Weight

778.06

Formula

C35H32ClF3N3O10P

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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CREB-IN-1 TFA
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HY-144318
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