BI-7273 | CAS#1883429-21-7 | BRD9 inhibitor

MedKoo Cat#: 406830 | Name: BI-7273

Description:

WARNING: This product is for research use only, not for human or veterinary use.

BI-7273 is a potent and selective BRD9 inhibitor. BI-7273 may be useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases.

Chemical Structure

BI-7273

CAS#1883429-21-7

Theoretical Analysis

MedKoo Cat#: 406830

Name: BI-7273

CAS#: 1883429-21-7

Chemical Formula: C20H23N3O3

Exact Mass: 353.1739

Molecular Weight: 353.42

Elemental Analysis: C, 67.97; H, 6.56; N, 11.89; O, 13.58

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 550.00	2 Weeks
200mg	USD 2,250.00	2 weeks

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Synonym

BI-7273; BI 7273; BI7273; I-BRD9; I-BRD 9; I-BRD-9

IUPAC/Chemical Name

4-(4-((dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

InChi Key

RBUYFHLQNPJMQM-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H23N3O3/c1-22(2)11-17-18(25-4)8-13(9-19(17)26-5)16-12-23(3)20(24)15-10-21-7-6-14(15)16/h6-10,12H,11H2,1-5H3

SMILES Code

O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C(OC)=C2)C3=CC=NC=C13

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

BI-7273 is a BRD9 inhibitor with an IC50 of 19 nM.

In vitro activity:

The cellular response to BRD9 inhibition was assessed in a broad cancer cell line panel. Treatment of the panel with BI-7273 resulted in decreased proliferation in the murine AML RN2 cell line. As observed from the phenotype of murine cells exposed to BI-7273, BRD9 inhibition translated into a potent but only partial inhibition of MYC expression in AML cell lines (Supporting Information Figure 32a–d). Reference: J Med Chem. 2016 May 26;59(10):4462-75. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4885110/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	26.7	75.55
	Ethanol	35.0	99.06
	PBS (pH 7.2)	0.1	0.28

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 353.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75. doi: 10.1021/acs.jmedchem.5b01865. Epub 2016 Mar 10. PMID: 26914985; PMCID: PMC4885110.

In vitro protocol:

In vivo protocol:

TBD

1: Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, Rogers C, Rumpel K, Schaaf O, Steurer S, Tallant C, Vakoc CR, Zeeb M, Zoephel A, Pearson M, Boehmelt G, McConnell D. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75. doi: 10.1021/acs.jmedchem.5b01865. Epub 2016 Mar 10. PubMed PMID: 26914985; PubMed Central PMCID: PMC4885110.