1. Epigenetics
  2. Epigenetic Reader Domain
  3. AZD5153 6-Hydroxy-2-naphthoic acid

AZD5153 6-Hydroxy-2-naphthoic acid (Synonyms: AZD-5153 HNT salt)

Cat. No.: HY-100653A Purity: 99.95%
Handling Instructions

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.

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

AZD5153 6-Hydroxy-2-naphthoic acid Chemical Structure

AZD5153 6-Hydroxy-2-naphthoic acid Chemical Structure

CAS No. : 1869912-40-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 212 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 246 In-stock
Estimated Time of Arrival: December 31
25 mg USD 528 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1560 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.

IC50 & Target

IC50: 1.7 nM (BRD4)[1]

In Vitro

AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153[1].

In Vivo

Administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 treatment markedly impacts transcriptional programs of MYC, E2F, and mTOR[1].

Clinical Trial
Molecular Weight

667.75

Formula

C₃₆H₄₁N₇O₆

CAS No.

1869912-40-2

SMILES

O=C(C1=CC=C2C=C(O)C=CC2=C1)O.O=C3N(C)CCN(CCOC4=CC=C(C5CCN(C6=NN7C(C=C6)=NN=C7OC)CC5)C=C4)[[email protected]@H]3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (50.92 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4976 mL 7.4878 mL 14.9757 mL
5 mM 0.2995 mL 1.4976 mL 2.9951 mL
10 mM 0.1498 mL 0.7488 mL 1.4976 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: Mice are treated with either vehicle (0.5% hydroxymethylcellulose, 0.1% Tween80) or AZD5153 by oral gavage mini-pump infusion. For continuous administration of AZD5153, compound is solubilized in 20% v/v DMSO/60% v/v HP-B-CD in water, loaded into a mini pump and implanted subcutaneously in mice. Tumor fragments collected are snap frozen or fixed in 10% buffered formalin. Blood samples are collected from the same mice and stabilized in EDTA. Plasma concentrations are determined by liquid chromatography/tandem mass spectrometry method[1].

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

References

Purity: 99.95%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AZD5153AZD-5153 HNTAZD 5153AZD-5153Epigenetic Reader DomainInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZD5153 6-Hydroxy-2-naphthoic acid
Cat. No.:
HY-100653A
Quantity:
MCE Japan Authorized Agent: