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  3. OXFBD02

OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.

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

OXFBD02 Chemical Structure

OXFBD02 Chemical Structure

CAS No. : 1429129-68-9

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM[1].

IC50 & Target

BRD4(1)

382 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
786-0 GI50
27.1 μM
Compound: 1a; OXFBD02
Growth inhibition of human 786-0 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human 786-0 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
A498 GI50
1.58 μM
Compound: 1a; OXFBD02
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]
A549 IC50
> 10 μM
Compound: 8
Cytotoxicity against human A549 cells after 72 hrs by MTS assay
Cytotoxicity against human A549 cells after 72 hrs by MTS assay
[PMID: 23517011]
A549 GI50
22.4 μM
Compound: 1a; OXFBD02
Growth inhibition of human A549/ATCC cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human A549/ATCC cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
ACHN GI50
4.76 μM
Compound: 1a; OXFBD02
Growth inhibition of human ACHN cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human ACHN cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
BT-549 GI50
28.2 μM
Compound: 1a; OXFBD02
Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human BT549 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
CAKI-1 GI50
4.58 μM
Compound: 1a; OXFBD02
Growth inhibition of human CAKI-1 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human CAKI-1 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
CCRF-CEM GI50
14.8 μM
Compound: 1a; OXFBD02
Growth inhibition of human CCRF-CEM cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human CCRF-CEM cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
COLO 205 GI50
5.25 μM
Compound: 1a; OXFBD02
Growth inhibition of human COLO205 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human COLO205 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
DU-145 GI50
6.95 μM
Compound: 1a; OXFBD02
Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HCC 2998 GI50
8.55 μM
Compound: 1a; OXFBD02
Growth inhibition of human HCC2998 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HCC2998 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HCT-116 GI50
7.08 μM
Compound: 1a; OXFBD02
Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HCT-15 GI50
3.52 μM
Compound: 1a; OXFBD02
Growth inhibition of human HCT15 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HCT15 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HeLa IC50
> 100 μM
Compound: 8
Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay
Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay
[PMID: 23517011]
HL-60(TB) GI50
2.17 μM
Compound: 1a; OXFBD02
Growth inhibition of human HL-60(TB) cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HL-60(TB) cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HOP-62 GI50
4.89 μM
Compound: 1a; OXFBD02
Growth inhibition of human HOP62 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HOP62 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HOP-92 GI50
1.02 μM
Compound: 1a; OXFBD02
Growth inhibition of human HOP92 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HOP92 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
Hs-578T GI50
1.93 μM
Compound: 1a; OXFBD02
Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human Hs 578T cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
HT-29 GI50
4.54 μM
Compound: 1a; OXFBD02
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]
IGROV-1 GI50
23.2 μM
Compound: 1a; OXFBD02
Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
K562 GI50
8.69 μM
Compound: 1a; OXFBD02
Growth inhibition of human K562 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human K562 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
KM12 GI50
8.2 μM
Compound: 1a; OXFBD02
Growth inhibition of human KM12 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human KM12 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
LOX IMVI GI50
3.6 μM
Compound: 1a; OXFBD02
Growth inhibition of human LOXIMVI cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human LOXIMVI cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
M14 GI50
4.48 μM
Compound: 1a; OXFBD02
Growth inhibition of human M14 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human M14 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
Malme-3M GI50
28.9 μM
Compound: 1a; OXFBD02
Growth inhibition of human MALME-3M cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MALME-3M cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
MCF7 GI50
1.25 μM
Compound: 1a; OXFBD02
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]
MDA-MB-231 GI50
3.92 μM
Compound: 1a; OXFBD02
Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
MDA-MB-435 GI50
3.48 μM
Compound: 1a; OXFBD02
Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
MDA-MB-468 GI50
1.89 μM
Compound: 1a; OXFBD02
Growth inhibition of human MDA-MB-468 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MDA-MB-468 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
MOLT-4 GI50
17.9 μM
Compound: 1a; OXFBD02
Growth inhibition of human MOLT4 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MOLT4 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
MV4-11 IC50
0.794 μM
Compound: 8
Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay
Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay
[PMID: 23517011]
NCI/ADR-RES GI50
6.32 μM
Compound: 1a; OXFBD02
Growth inhibition of human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
NCI-H1975 IC50
> 10 μM
Compound: 8
Cytotoxicity against human NCI-H1975 cells after 72 hrs by MTS assay
Cytotoxicity against human NCI-H1975 cells after 72 hrs by MTS assay
[PMID: 23517011]
NCI-H226 GI50
21.3 μM
Compound: 1a; OXFBD02
Growth inhibition of human NCI-H226 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H226 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
NCI-H322M GI50
8.41 μM
Compound: 1a; OXFBD02
Growth inhibition of human NCI-H322M cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H322M cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
NCI-H460 GI50
25.1 μM
Compound: 1a; OXFBD02
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
NCI-H522 GI50
27 μM
Compound: 1a; OXFBD02
Growth inhibition of human NCI-H522 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H522 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
OVCAR-3 GI50
6.64 μM
Compound: 1a; OXFBD02
Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
OVCAR-4 GI50
6.35 μM
Compound: 1a; OXFBD02
Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
OVCAR-5 GI50
31.8 μM
Compound: 1a; OXFBD02
Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
OVCAR-8 GI50
8.33 μM
Compound: 1a; OXFBD02
Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
RPMI-8226 GI50
1.94 μM
Compound: 1a; OXFBD02
Growth inhibition of human RPMI8226 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human RPMI8226 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
RXF 393 GI50
17.2 μM
Compound: 1a; OXFBD02
Growth inhibition of human RXF393 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human RXF393 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SF-268 GI50
39.3 μM
Compound: 1a; OXFBD02
Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SF-295 GI50
7.31 μM
Compound: 1a; OXFBD02
Growth inhibition of human SF295 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SF295 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SF-539 GI50
4.56 μM
Compound: 1a; OXFBD02
Growth inhibition of human SF539 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SF539 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SK-MEL-2 GI50
23.5 μM
Compound: 1a; OXFBD02
Growth inhibition of human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SK-MEL-28 GI50
9.15 μM
Compound: 1a; OXFBD02
Growth inhibition of human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SK-MEL-5 GI50
5.95 μM
Compound: 1a; OXFBD02
Growth inhibition of human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SK-OV-3 GI50
7.01 μM
Compound: 1a; OXFBD02
Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SN12C GI50
3.99 μM
Compound: 1a; OXFBD02
Growth inhibition of human SN12C cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SN12C cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SNB-19 GI50
5.69 μM
Compound: 1a; OXFBD02
Growth inhibition of human SNB19 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SNB19 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SNB-75 GI50
0.423 μM
Compound: 1a; OXFBD02
Growth inhibition of human SNB75 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SNB75 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SR GI50
1.01 μM
Compound: 1a; OXFBD02
Growth inhibition of human SR cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SR cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
SW-620 GI50
24.5 μM
Compound: 1a; OXFBD02
Growth inhibition of human SW620 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SW620 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
T47D GI50
7.7 μM
Compound: 1a; OXFBD02
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
TK-10 GI50
1.08 μM
Compound: 1a; OXFBD02
Growth inhibition of human TK10 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human TK10 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
U-251 GI50
15 μM
Compound: 1a; OXFBD02
Growth inhibition of human U251 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human U251 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
U2OS IC50
> 100 μM
Compound: 8
Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay
Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay
[PMID: 23517011]
UACC-257 GI50
4.66 μM
Compound: 1a; OXFBD02
Growth inhibition of human UACC257 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human UACC257 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
UO-31 GI50
4.58 μM
Compound: 1a; OXFBD02
Growth inhibition of human UO31 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human UO31 cells after 48 hrs by sulforhodamine B assay
[PMID: 29776834]
Molecular Weight

295.33

Formula

C18H17NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1=CC=CC=C1)C2=CC(O)=CC(C3=C(C)ON=C3C)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (338.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3860 mL 16.9302 mL 33.8604 mL
5 mM 0.6772 mL 3.3860 mL 6.7721 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3860 mL 16.9302 mL 33.8604 mL 84.6511 mL
5 mM 0.6772 mL 3.3860 mL 6.7721 mL 16.9302 mL
10 mM 0.3386 mL 1.6930 mL 3.3860 mL 8.4651 mL
15 mM 0.2257 mL 1.1287 mL 2.2574 mL 5.6434 mL
20 mM 0.1693 mL 0.8465 mL 1.6930 mL 4.2326 mL
25 mM 0.1354 mL 0.6772 mL 1.3544 mL 3.3860 mL
30 mM 0.1129 mL 0.5643 mL 1.1287 mL 2.8217 mL
40 mM 0.0847 mL 0.4233 mL 0.8465 mL 2.1163 mL
50 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6930 mL
60 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4109 mL
80 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0581 mL
100 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8465 mL
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  • 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.

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Product Name:
OXFBD02
Cat. No.:
HY-103297
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