ChemicalBook > CAS DataBase List > BI-7273

BI-7273

Product Name: BI-7273
CAS No.: 1883429-21-7
Chemical Name: BI-7273
Synonyms: BI273;BI-7273;CS-2327;BI 7273;BI7273;BI-7273, 10 mM in DMSO;inhibit,Inhibitor,Epigenetic Reader Domain,BI7273,BI-7273,BI 7273;4-(4-((dimethylamino)methyl)-2,6-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one;2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-
CBNumber: CB53128809
Molecular Formula: C20H23N3O3
Formula Weight: 353.41
MOL File: 1883429-21-7.mol

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BI-7273 Property

Boiling point:: 509.2±50.0 °C(Predicted)
Density: 1.189±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥35.3 mg/mL in DMSO with gentle warming; ≥1.99 mg/mL in EtOH with ultrasonic; ≥8.74 mg/mL in H2O
form: solid
pka: 8.32±0.28(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 20311
Product name: BI-7273
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 20311
Product name: BI-7273
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 20311
Product name: BI-7273
Purity: ≥98%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 20311
Product name: BI-7273
Purity: ≥98%
Packaging: 25mg
Price: $573
Updated: 2024/03/01

ChemScene

Product number: CS-5887
Product name: BI-7273
Purity: 99.98%
Packaging: 50mg
Price: $720
Updated: 2021/12/16

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BI-7273 Chemical Properties,Usage,Production

Description

BI-7273 is a potent BRD9 bromodomain inhibitor (K_d = 15.4 nM; IC₅₀ = 19 nM) that less effectively inhibits the functionally and structurally related BRD7 bromodomain (IC₅₀ = 117 nM). It is without effect against the bromodomains of BRD2 and BRD4, as well as a panel of kinases. BI-7273 inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC₅₀ = 1.4 μM).

Uses

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

in vitro

bi-7273 was previously demonstrated to mimic genetic perturbation of brd9. bi-7273 could also target brd7 bd, a bd protein that was found in a subclass of swi/snf remodelling complexes sharing high sequence homology with brd9. in addition, bi-7273 was able to form an additional positive interaction with the carbonyl of asn100 in brd9. furthermore, bi-7273 showed no measurable activity against bet family bds even up to a concentration of 100 μm in the biochemical alpha assay [1].

in vivo

in order to explore the potential of bi-7273 as in-vivo chemical probe, female bomtac:nmrifoxn1nu mice was orally administered two doses at 20 and 180 mg/ kg and the concentration of bi-7273 in plasma over time was measured. results showed that dose-dependent but nonlinear auc was observed for bi-7273, achieving exposure that was higher compared to the ec50 level determined for bi-7273 in proliferation assays with eol-1 cells [1].

IC 50

19 and 117 nm for brd9 and brd7, respectively.

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.

BI-7273 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI-7273 Suppliers

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1883429-21-7, BI-7273Related Search:

BI-7273

BI273

BI 7273;BI7273

CS-2327

2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-

inhibit,Inhibitor,Epigenetic Reader Domain,BI7273,BI-7273,BI 7273

4-(4-((dimethylamino)methyl)-2,6-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

BI-7273, 10 mM in DMSO

1883429-21-7

1883429-21-9