1. Epigenetics
  2. Epigenetic Reader Domain
  3. OXFBD04

OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.

For research use only. We do not sell to patients.

OXFBD04 Chemical Structure

OXFBD04 Chemical Structure

CAS No. : 2231747-03-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 319 In-stock
Solution
10 mM * 1 mL in DMSO USD 319 In-stock
Solid
5 mg USD 290 In-stock
10 mg USD 470 In-stock
50 mg USD 1300 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity[1].

IC50 & Target[1]

BRD4

166 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A498 GI50
4.88 μM
Compound: 9j
Growth inhibition of human A498 cells after 48 hrs by SRB assay
Growth inhibition of human A498 cells after 48 hrs by SRB assay
[PMID: 29776834]
HT-29 GI50
4.4 μM
Compound: 9j
Growth inhibition of human HT-29 cells after 48 hrs by SRB assay
Growth inhibition of human HT-29 cells after 48 hrs by SRB assay
[PMID: 29776834]
MCF7 GI50
1.4 μM
Compound: 9j
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
[PMID: 29776834]
In Vitro

OXFBD04 (0.01-100 μM; 48 hours) inhibits cancer cell lines growth[1].
OXFBD04 (10 µM; for 10, 24, or 48 hours) induces MYC suppression in MCF7 breast cancer cells[1].

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

Cell Viability Assay[1]

Cell Line: A498 (renal), HT-29 (colon), and MCF7 (breast) cancer cell lines
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 48 hours
Result: Inhibited cancer cell lines growth.
In Vivo

OXFBD04 has optimised physicochemical properties (LE=0.43; LLE=5.74; SFI=5.96), and good metabolic stability (t1/2=388 min). OXFBD04 has CLint of 3.57 µL/min/mg[1].

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

Molecular Weight

296.32

Formula

C17H16N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1=CC(O)=CC(C2=C(C)ON=C2C)=C1)C3=CC=CN=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (843.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3747 mL 16.8736 mL 33.7473 mL
5 mM 0.6749 mL 3.3747 mL 6.7495 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3747 mL 16.8736 mL 33.7473 mL 84.3682 mL
5 mM 0.6749 mL 3.3747 mL 6.7495 mL 16.8736 mL
10 mM 0.3375 mL 1.6874 mL 3.3747 mL 8.4368 mL
15 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
20 mM 0.1687 mL 0.8437 mL 1.6874 mL 4.2184 mL
25 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
30 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
40 mM 0.0844 mL 0.4218 mL 0.8437 mL 2.1092 mL
50 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
60 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
80 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0546 mL
100 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
OXFBD04
Cat. No.:
HY-135236
Quantity:
MCE Japan Authorized Agent: