BI-7273
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406830

CAS#: 1883429-21-7

Description: 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

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BI-7273
CAS# 1883429-21-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406830
Name: BI-7273
CAS#: 1883429-21-7
Chemical Formula: C20H23N3O3
Exact Mass: 353.17
Molecular Weight: 353.422
Elemental Analysis: C, 67.97; H, 6.56; N, 11.89; O, 13.58

Price and Availability

Size Price Availability Quantity
5mg USD 350 2 weeks
10mg USD 550 2 Weeks
200mg USD 2250 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

Solubility Data

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

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.

Recalculate based on batch purity %
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: 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 vivo protocol: TBD

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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.