BI-9564 | CAS#1883429-22-8 | BRD9 inhibitor

MedKoo Cat#: 406829 | Name: BI-9564

Description:

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

BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 µM, respectively). BI-9564 is 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-9564

CAS#1883429-22-8

Theoretical Analysis

MedKoo Cat#: 406829

Name: BI-9564

CAS#: 1883429-22-8

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
50mg	USD 750.00	2 Weeks
100mg	USD 1,350.00	2 Weeks
200mg	USD 2,250.00	2 Weeks

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Synonym

BI-9564; BI 9564; BI9564.

IUPAC/Chemical Name

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

InChi Key

BJFSUDWKXGMUKA-UHFFFAOYSA-N

InChi Code

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

SMILES Code

O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)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-9564 is a BRD9/BRD7 bromodomains inhibitor with IC50s of 75 nM and 3.4 μM, respectively.

In vitro activity:

Target engagement in the cell was demonstrated in a semiquantitative FRAP assay using a green fluorescent protein–BRD9 fusion protein expressed in U2OS cells. BI-9564 showed inhibition of BRD9 in cells at 100 nM. The cellular response to BRD9 inhibition was assessed in a broad cancer cell line panel. Treatment of the panel with BI-9564 resulted in selective growth inhibition of a significant proportion of AML cell lines tested (Supporting Information Figure 31). Reference: J Med Chem. 2016 May 26;59(10):4462-75. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4885110/

In vivo activity:

In order to evaluate the effect of BI-9564 in vivo, EOL-1 cells, stably transduced with a luciferase-expressing vector to allow continuous assessment of tumor load by bioluminescence, were injected in the tail vein of CIEA-NOG mice. Oral treatment with 180 mg/kg of BI-9564 was initiated on day 5 and applied daily (q.d.) with an interruption at days 18 and 19. A significant (p = 0.0086) reduction in tumor growth (measured in average radiance [p/s/cm2/sr]) compared to that of controls was observed on day 18, resulting in a median tumor growth inhibition (TGI) value of 52% (Figure 6a). Imaging data on day 18 provided evidence of a significantly reduced disease burden (Figure 6b) in mice treated with BI-9564. Reference: J Med Chem. 2016 May 26;59(10):4462-75. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4885110/

	Solvent	mg/mL	mM
Solubility
	DMF	5.0	14.15
	DMF:PBS (pH 7.2) (1:1)	0.5	1.41
	DMSO	5.4	15.39
	Ethanol	9.0	25.47

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:

1: Karim RM, Schönbrunn E. An Advanced Tool To Interrogate BRD9. J Med Chem. 2016 May 26;59(10):4459-61. doi: 10.1021/acs.jmedchem.6b00550. Epub 2016 Apr 27. PubMed PMID: 27120693. 2: 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.