GLPBio

AZD5153 6-Hydroxy-2-naphthoic acid

Catalog No.: GC35448Purity:>99.50%
COASDSData Sheet
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.

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AZD5153 6-Hydroxy-2-naphthoic acid
Cas No.: 1869912-40-2
10mM (in 1mL DMSO)In Stock
$123.00
1
1mgIn Stock
$38.00
1
5mgIn Stock
$84.00
1
10mgIn Stock
$138.00
1
25mgIn Stock
$235.00
1
50mgIn Stock
$350.00
1
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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: 1.7 nM (BRD4)[1]

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].

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].

[1]. 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.

Protocol

Animal experiment:

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].

References:

[1]. 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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

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)[C@@H]3C
Molecular Formula
C36H41N7O6
Molecular Weight
667.75
Solubility
DMSO: ≥ 34 mg/mL (50.92 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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