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666-15 (Synonyms: Compound 3i)

Catalog No.GC32689

An inhibitor of CREB-mediated gene transcription

Products are for research use only. Not for human use. We do not sell to patients.

666-15 Chemical Structure

Cas No.: 1433286-70-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$141.00
In stock
5mg
$104.00
In stock
10mg
$167.00
In stock
25mg
$351.00
In stock
50mg
$585.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Cells are plated into 96-well plates and the cells are allowed to attach to the bottom of the plates overnight. Then the cells are treated with different concentrations of different drugs (666-15) for 72 h. The media are removed, and MTT reagent in complete tissue culture media is added to each well and incubated at 37 °C for 3 h. The incubation media are removed and 100 μL of DMSO is added to each well. The absorbance of the formed purple formazan solution is read at 570 nm using a plate reader[1].

Animal experiment:

Mice: 666-15 is dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in water. Each 6- to 8-week old BALB/c nude mouse is inoculated subcutaneously at the right flank with MDA-MB-468 cells. Mice are treated with either vehicle or 666-15 at 10 mg/kg. The mice are treated once a day for 5 consecutive days a week, and the treatment lasted for 5 weeks[1].

References:

[1]. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J Med Chem. 2015 Jun 25;58(12):5075-87.

Background

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.

666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC50 of 18.27 μM. 666-15 inhibits CREB's transcription activity in living cells independent of direct CREB or CBP binding interaction. 666-15 is very potent in inhibiting CREB's transcription activity. 666-15 also inhibits endogenous CREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2)[1].

Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice. The tumor growth in the mice treated with 666-15 is efficaciously inhibited with complete tumor stasis. During the same period, the tumor volume in the vehicle-treated group is more than tripled. The body weights of 666-15-treated animals and vehicle-treated ones are indistinguishable from each other during the entire treatment period[1].

[1]. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J Med Chem. 2015 Jun 25;58(12):5075-87.

Chemical Properties

Cas No. 1433286-70-4 SDF
Synonyms Compound 3i
Canonical SMILES O=C(NC1=CC=C(Cl)C=C1O)C2=CC3=CC=CC=C3C=C2OCCNC(C4=C(OCCCN)C=C(C=CC=C5)C5=C4)=O.Cl
Formula C33H31Cl2N3O5 M.Wt 620.52
Solubility DMSO : ≥ 30 mg/mL (48.35 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6116 mL 8.0578 mL 16.1155 mL
5 mM 0.3223 mL 1.6116 mL 3.2231 mL
10 mM 0.1612 mL 0.8058 mL 1.6116 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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