ChemicalBook CAS DataBase List 2080306-23-4

2080306-23-4

Name	BAY 299
CAS	2080306-23-4
Molecular Formula	C25H23N3O4
MDL Number	MFCD30480933
Molecular Weight	429.47
MOL File	2080306-23-4.mol

Chemical Properties

Boiling point	688.7±55.0 °C(Predicted)
density	1.377±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:30.0(Max Conc. mg/mL);69.85(Max Conc. mM) DMF:30.0(Max Conc. mg/mL);69.85(Max Conc. mM)
form	A crystalline solid
pka	14.98±0.10(Predicted)
color	Light yellow to yellow

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning

Hazard Information

Description

BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC₅₀ = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC₅₀ = 13 nM). BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.

Uses

BAY 299, is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1, also known as BRPF2, and a strong inhibitor of TAF1/TAF1L BD2. These proteins play important roles in transcription regulation.

in vivo

Studies of the in vivo pharmacokinetic properties of BAY-299 in rat reveal that blood clearance is low (ca. 17% of hepatic blood flow), volume of distribution in steady-state high, terminal half-life long to very long (t_1/2=10 h), and bioavailability high (F=73%). In vivo blood clearance is as anticipated based on rat liver microsome values but lower than expected based on hepatocyte data^[1].

IC 50

BRPF2 BD: 67 nM (IC₅₀); BRPF1 BD: 3150 nM (IC₅₀); BRPF3 BD: 5550 nM (IC₅₀); TAF1 BD2: 8 nM (IC₅₀); TAF1L BD2: 106 nM (IC₅₀)

storage

Store at -20°C

References

[1] MONTSERRAT PéREZ-SALVIA M E. Bromodomain inhibitors and cancer therapy: From structures to applications[J]. Epigenetics, 2016, 12 1: 323-339. DOI: 10.1080/15592294.2016.1265710

Spectrum Detail

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