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AZD-5153 HNT salt

Cat. No. M9026

All AbMole products are for research use only, cannot be used for human consumption.

AZD-5153 HNT salt Structure
Synonym:

AZD5153

Size Price Availability Quantity
5mg USD 158  USD158 In stock
10mg USD 270  USD270 In stock
25mg USD 530  USD530 In stock
50mg USD 940  USD940 In stock
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Quality Control & Documentation
Biological Activity

AZD-5153 HNT salt is a 6-hydroxy-2-naphthoic acid salt of AZD-5153. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153.

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 modulates MYC and HEXIM1 in AML xenograft tumors and human whole blood. AZD5153 treatment markedly impacts transcriptional programs of MYC, E2F and mTOR.

Protocol (for reference only)
Cell Experiment
Cell lines MV-4-11, MM.1S, and K562 cells
Preparation method Apoptosis was analyzed by flow cytometry using CellEvent Caspase 3/7 Green detection reagent. MV-4-11, MM.1S, and K562 cells were pretreated with AZD5153 or I-BET762 for 48 hours in culture media. Cells were collected and stained with 5 μmol/L final concentration of CellEvent for 30 minutes at 37°C. Flow cytometry was done on a BD Fortessa using the Blue laser and FITC filter set.
Concentrations
Incubation time 48 h
Animal Experiment
Animal models Female CB17 SCID and SCID beige mice
Formulation 0.5% hydroxymethylcellulose, 0.1% Tween80 (oral); 20% v/v DMSO/60% v/v HP-B-CD in water (s.c)
Dosages
Administration by oral gavage mini-pump infusion or s.c
Chemical Information
Molecular Weight 667.75
Formula C25H33N7O3.C11H8O3
CAS Number 1869912-40-2
Solubility (25°C) DMSO: ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Collins TA, et al. CPT Pharmacometrics Syst Pharmacol. Translational Modeling of Drug-Induced Myelosuppression and Effect of Pretreatment Myelosuppression for AZD5153, a Selective BRD4 Inhibitor.

[2] Yeh TC, et al. Clin Cancer Res. Identification of CCR2 and CD180 as Robust Pharmacodynamic Tumor and Blood Biomarkers for Clinical Use with BRD4/BET Inhibitors.

[3] Rhyasen GW, et al. Mol Cancer Ther. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.

[4] Bradbury RH, et al. J Med Chem. Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).

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Keywords: AZD-5153 HNT salt, AZD5153 supplier, Epigenetic Reader Domain, inhibitors, activators

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