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BI-9564 

Cat. No.: HY-100352 Purity: 99.55%
Handling Instructions

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.

For research use only. We do not sell to patients.

BI-9564 Chemical Structure

BI-9564 Chemical Structure

CAS No. : 1883429-22-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 75 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
2 mg USD 72 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1020 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg USD 1920 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & 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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.2830 mL 1.4148 mL 2.8296 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

BI-9564 is formulated with 0.5% Natrosol.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

353.41

Formula

C₂₀H₂₃N₃O₃

CAS No.

1883429-22-8

SMILES

CN(C)CC1=CC(OC)=C(C(C2=C3C=NC=C2)=CN(C)C3=O)C=C1OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 7.2 mg/mL (Need warming)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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BI-9564
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HY-100352
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