BI-7273

Name: BI-7273
Brand: MedChemExpress
SKU: HY-100351
Rating: 5.0 (1 reviews)

Cat. No.: HY-100351 Purity: 99.75%: Data Sheet
COA

SDS
Handling Instructions
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BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC₅₀ and a K_d of 19 and 0.75 nM; also shows high effect on BRD7, with an IC₅₀ and a K_d of 117 nM and 0.3 nM.

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

The BI-7273 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

CAS No. : 1883429-21-7

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BI-7273:

BI-7273 (Standard) Get quote

1 Publications Citing Use of MCE BI-7273

•Noncoding RNA. 2025 Apr 29;11(3):33.

RT-PCR

: BI-7273 purchased from MedChemExpress. Usage Cited in: Noncoding RNA. 2025 Apr 29;11(3):33.; Treatment with Bi7273 (5 μM) is ineffective in modulating cell adhesion molecules E-cadherin and β4 integrin, while it can downregulate a known BRD7/BRD9 target gene like CCND1.

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Biological Activity
Protocol
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 19 nM (BRD9), 117 nM (BRD7)^[1]
Kd: 0.75 nM (BRD9), 0.3 nM (BRD7)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A204	IC₅₀	0.3717 μM Compound: 1a;BI-7273	Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay	[PMID: 30540463]
EOL1	EC₅₀	1400 nM Compound: 1; BI-7273	Antiproliferative activity against human EOL-1 cells by cell titre glo assay Antiproliferative activity against human EOL-1 cells by cell titre glo assay	[PMID: 26914985]
EOL1	IC₅₀	0.08926 μM Compound: 1a;BI-7273	Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay	[PMID: 30540463]
G-401	IC₅₀	4.9 μM Compound: 3; BI-7273	Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay Inhibition of cell viability in human G-401 cells incubated for 4 days by CellTiter-Glo luminescent cell viability assay	[PMID: 39132814]

In Vitro

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC₅₀ and a K_d of 19 and 0.75 nM; also shows high effect on BRD7, with an IC₅₀ and a K_d of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with K_ds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC₅₀ of 1400 nM^[1].

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

Molecular Weight

353.41

Formula

C₂₀H₂₃N₃O₃

CAS No.

1883429-21-7

Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC1=C(OC)C=C(C(C2=C3C=NC=C2)=CN(C)C3=O)C=C1OC

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 : 10 mg/mL (28.30 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	2.8296 mL	14.1479 mL	28.2957 mL
5 mM	0.5659 mL	2.8296 mL	5.6591 mL
10 mM	0.2830 mL	1.4148 mL	2.8296 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 1 mg/mL (2.83 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.83 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 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)

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

Purity: 99.75%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (253 KB) RP-HPLC (252 KB) MS (206 KB)

Handling Instructions (2659 KB)

References

[1]. Laetitia J Martin, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75. [Content Brief]

[2]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.

Kinase Assay ^[1]	His-tagged BRD9 is immobilized to a density of 2000-4000 RUs on flow cells 3 and 4 of a Biacore NTA-chip. Carbonic anhydrase II is immobilized at a similar density on flow cell 2 and a blank reference surface is generated on flow cell 1. The buffer is then switched to assay buffer (HBS-P+ = 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05 % P20 + 5 % DMSO) and the chip equilibrated for several hours before use for K_d determinations. To be able to correct for differences in bulk solvent refractive index caused by small variations in the DMSO concentration solvent correction samples are included at the beginning and end of the run. Compounds (BI-7273, etc.) are injected in concentration series (1:1 dilutions, 7 different concentrations), starting with a maximum concentration that is approximately 10-20-fold higher than the expected K_d. The concentration series are prepared in 96-well plates. In the case that the dilution window chosen for a particular compound does not appropriately bracket the K_d of the compound the measurement is repeated with an optimized starting concentration. Positive and negative control samples are included at regular intervals to be able to monitor the performance of the assay. CBS is used as a positive control for carbonic anhydrase II to check for integrity of the reference protein at regular intervals. To correct for the excluded volume effect a DMSO calibration series is prepared and the calibration samples are measured at the beginning and end of each run. K_d values are determined and averaged^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are grown in 50 µL medium for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound (BI-7273, etc.) before measuring viability via cellular ATP levels using the cell titer glow assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Laetitia J Martin, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75. [Content Brief] [2]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8296 mL	14.1479 mL	28.2957 mL	70.7394 mL
	5 mM	0.5659 mL	2.8296 mL	5.6591 mL	14.1479 mL
	10 mM	0.2830 mL	1.4148 mL	2.8296 mL	7.0739 mL
	15 mM	0.1886 mL	0.9432 mL	1.8864 mL	4.7160 mL
	20 mM	0.1415 mL	0.7074 mL	1.4148 mL	3.5370 mL
	25 mM	0.1132 mL	0.5659 mL	1.1318 mL	2.8296 mL

BI-7273 Related Classifications

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:

BI-72731883429-21-7BI7273BI 7273Epigenetic Reader DomainInhibitorinhibitorinhibit

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BI-7273

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Complete Stock Solution Preparation Table

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