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  3. Epigenetic Reader Domain
  4. CREB-IN-1 TFA

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

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CREB-IN-1 TFA Chemical Structure

CREB-IN-1 TFA Chemical Structure

CAS No. : 2912285-84-6

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CREB-IN-1 TFA Related Antibodies

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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].

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

CREB-IN-1 TFA Related Antibodies

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].

MedChemExpress (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
CAS No.
SMILES

NCCCOC1=C(C=C2C=CC=CC2=C1)C(NCCOC3=CC4=CC=CC=C4C=C3C(NC5=CC=C(C=C5OP(O)(O)=O)Cl)=O)=O.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CREB-IN-1 TFA Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CREB-IN-12912285-84-6Epigenetic Reader Domainbreast cancerorally activeHEK 293T cellsMDA-MB-231 cellsMDA-MB-468 cellsphosphateInhibitorinhibitorinhibit

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