BI-9564

Modify Date: 2024-01-02 11:47:45

BI-9564 structure	Common Name	BI-9564
	CAS Number	1883429-22-8	Molecular Weight	353.415
	Density	1.2±0.1 g/cm3	Boiling Point	519.9±50.0 °C at 760 mmHg
	Molecular Formula	C₂₀H₂₃N₃O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	268.3±30.1 °C

Use of BI-9564

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

Name	4-{4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl}-2-methyl-2,7-naphthyridin-1(2H)-one
Synonym	More Synonyms

Description	BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
Target	Kd: 20 nM (BRD9)
In Vitro	BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM[1]. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells[2].
In Vivo	BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML[1].
Cell Assay	Cells are grown in 50 µL medium as specified by the supplier 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 before measuring viability via cellular ATP levels using the cell titer glow assay.
Animal Admin	Female CIEA-NOG mice are engrafted intravenously with 1×107 EOL-1 AML cells stably expressing luciferase and GFP. Following injection of the cells animals are randomized based on body weight (n=10/group). Treatment starts on day 5 with either 0.5% Natrosol or BI-9564 formulated with 0.5% Natrosol. All doses are calculated relative to the mouse body weight on the treatment day. BI-9564 and the vehicle control are administered orally with a dosing volume of 10 mL/kg body weight. BI-9564 is administered daily from day 5 until 17 and from day 20 until 22. Dosing is interrupted on day 18 for two days as one mouse in the treatment group reaches -15% body weight loss. Tumour load is measured 2-3 times weekly based on bioluminescence imaging. The following scoring system is used: score 0, no clinical signs; score 1, tail or hind limb weakness. Animals are sacrificed based on severity criteria including appearance of paralysis score 1 and/or body weight loss exceeding -18%. In S54 this tumor mouse model body weight changes can occur due to increased tumor load or due to intolerability.
References	[1]. 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. [2]. Rezaul M. Karim, et al. An Advanced Tool To Interrogate BRD9. J. Med. Chem., 2016, 59 (10), pp 4459-4461

Density	1.2±0.1 g/cm3
Boiling Point	519.9±50.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₃N₃O₃
Molecular Weight	353.415
Flash Point	268.3±30.1 °C
Exact Mass	353.173950
LogP	2.05
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.590
Storage condition	-20℃

4-{4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl}-2-methyl-2,7-naphthyridin-1(2H)-on

2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-

4-{4-[(Diméthylamino)méthyl]-2,5-diméthoxyphényl}-2-méthyl-2,7-naphtyridin-1(2H)-one

4-{4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl}-2-methyl-2,7-naphthyridin-1(2H)-one

BI-9564

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: BI-9564
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: BI-9564
Price: $500.0/100mg $1000.0/250mg $2000.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: BI-9564
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

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Price: $75/10mM*1mLinDMSO

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BI-9564

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