AZD5153 HNT salt

This product is for research use only, not for human use. We do not sell to patients.

AZD5153 HNT salt
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500mg$2800Check With Us
1g$4200Check With Us

Cat #: V2765 CAS #: 1869912-40-2 Purity ≥ 98%

Description: AZD-5153 HNT salt, the 6-Hydroxy-2-naphthoic acid salt form of AZD5153, is a potent, selective, and orally available BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with pKi of 8.3 for BRD4.

References: Rhyasen GW, et al. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2563-2574.

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Molecular Weight (MW)667.75
Molecular FormulaC25H33N7O3.C11H8O3
CAS No.1869912-40-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mL (149.75 mM)r
Water: <1 mg/mLr
Ethanol: 27 mg/mL warmed (40.43 mM)
SMILES CodeO=C1N(C)CCN(CCOC2=CC=C(C3CCN(C4=NN5C(C=C4)=NN=C5OC)CC3)C=C2)[C@@H]1C.O=C(O)C6=CC=C7C=C(O)C=CC7=C6
SynonymsAZD5153; AZD 5153; AZD-5153 6-Hydroxy-2-naphthoic acid; AZD-5153; AZD-5153 6-hydroxy-2-naphthoate. AZD-5153 HNT salt.
ProtocolIn VitroAZD5153 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.
In VivoAdministration 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.4976 mL7.4878 mL14.9757 mL29.9513 mL
5mM0.2995 mL1.4976 mL2.9951 mL5.9903 mL
10mM0.1498 mL0.7488 mL1.4976 mL2.9951 mL
20mM0.0749 mL0.3744 mL0.7488 mL1.4976 mL
Quality Control Documentation
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: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.