2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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。

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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 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

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

CREB-IN-1 TFA 相关抗体:

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].

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%.
分子量

778.06

Formula

C35H32ClF3N3O10P
CAS 号
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.
纯度 & 产品资料
参考文献

CREB-IN-1 TFA 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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产品名称：
CREB-IN-1 TFA
目录号：
HY-144318
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