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AZD5153 6-Hydroxy-2-naphthoic acid

Catalog No. T3504 CAS 1869912-40-2

Synonyms: AZD5153, AZD-5153 HNT salt

AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor used in cancer treatments.

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AZD5153 6-Hydroxy-2-naphthoic acid Chemical Structure

AZD5153 6-Hydroxy-2-naphthoic acid, CAS 1869912-40-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
5 mg	In stock	$ 129.00
10 mg	In stock	$ 223.00
25 mg	In stock	$ 479.00
50 mg	In stock	$ 691.00
100 mg	In stock	$ 983.00
500 mg	In stock	$ 1,960.00
1 mL * 10 mM (in DMSO)	In stock	$ 189.00

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Purity: 100%

Purity: 98.36%

Purity: 98.18%

Purity: 98%

Purity: 97.2%

Biological Description

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Storage & Solubility Information

Description	AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor used in cancer treatments.
Targets&IC50	FL-BRD4:5 nM
In vitro	AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Of note, mTOR pathway modulation is associated with cell line sensitivity to AZD5153. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nmol/L. AZD5153 efficiently downregulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153. AML, MM, and DLBCL cell lines are highly sensitive to AZD5153.
In vivo	AZD5153 modulates MYC and HEXIM1 in AML xenograft tumors and human whole blood. 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 is administered orally to mice bearing MV-4-11 xenografts, and pharmacodynamic activity (intratumoral levels of c-Myc) is measured at 2, 4, and 8 h postdose. A considerable decrease in c-Myc expression is observed out to 8 h post dose at free plasma levels of compound <0.2 μM. This decrease in c-Myc expression after treatment with AZD5153 is consistent with other published BET inhibitors.
Cell Research	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. (Only for Reference)

Synonyms	AZD5153, AZD-5153 HNT salt
Molecular Weight	667.75
Formula	C25H33N7O3·C11H8O3
CAS No.	1869912-40-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 26 mg/mL (38.9 mM)

DMSO: 93 mg/mL (139.3 mM)

References and Literature

1. Rhyasen GW, et al. Mol Cancer Ther. 2016, 15(11):2563-2574. 2. Bradbury RH, et al. J Med Chem. 2016, 59(17):7801-17.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Histone Modification Compound Library Epigenetics Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Aging Compound Library

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Keywords

AZD5153 6-Hydroxy-2-naphthoic acid 1869912-40-2 Chromatin/Epigenetic Epigenetic Reader Domain AZD5153 AZD-5153 AZD-5153 HNT AZD5153 6 Hydroxy 2 naphthoic acid Inhibitor AZD-5153 HNT salt AZD5153 6Hydroxy2naphthoic acid AZD 5153 inhibit AZD-5153 6-Hydroxy-2-naphthoic acid inhibitor

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