CREB-IN-1 TFA

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CREB-IN-1 TFA 

CREB-IN-1 TFA 是一种有效的，具有口服活性的 CREB 抑制剂 (IC50=0.18 µM)。CREB-IN-1 TFA 能够抑制乳腺癌细胞的生长。

CREB-IN-1 TFA

CREB-IN-1 TFA Chemical Structure

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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[1].

IC50 & Target

IC50: 0.18 µM (CREB)[1]
体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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%.

分子量

778.06

Formula

C35H32ClF3N3O10P
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Peng J, et al. Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription. ACS Med Chem Lett. 2022; 13(3):388-395.

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