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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- CAS No.: 2912285-84-6
- 화학식: C35H32ClF3N3O10P
- 분자량:778.06
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
IC50: 0.18 µM (CREB)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | GI50 |
0.38 μM
Compound: 3
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Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
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[PMID: 35300089] |
| MDA-MB-468 | GI50 |
0.021 μM
Compound: 3
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Growth inhibition of human MDA-MB-468 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MDA-MB-468 cells incubated for 72 hrs by MTT assay
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[PMID: 35300089] |
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.
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Cell Line:HEK 293T cells
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Concentration:100 µM
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Incubation Time:24 hours
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Result:Inhibited CREB-mediated gene transcription with an IC50 of 0.18 µM.
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Cell Line:MDA-MB-231, MDA-MB-468 cells
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Concentration:100 µM
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Incubation Time:3 days
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Result:Showed potent activities in MDA-MB-231 (GI50 =0.38 µM) and MDA-MB-468 (GI50 =0.021 µM) cells.
In Vivo
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.
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Animal Model:Female C57BL/6 mice[1]
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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)
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Administration:Showed much improve oral bioavailability at 38%.
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Result:Showed much improve oral bioavailability at 38%.
Chemical Information
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CAS No. 2912285-84-6
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분자량 778.06
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화학식 C35H32ClF3N3O10P
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CREB-IN-1 TFA Related Classifications
HY-144318 Related Classifications
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