AZD5153 6-Hydroxy-2-naphthoic acid

Name: AZD5153 6-Hydroxy-2-naphthoic acid
Brand: MedChemExpress
SKU: HY-100653A
Rating: 5.0 (5 reviews)

製品番号: HY-100653A 純度: 99.51%: Data Sheet SDS COA 取扱説明書
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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

AZD5153 6-Hydroxy-2-naphthoic acid 構造式

CAS 番号 : 1869912-40-2

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 232	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 232	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$158	在庫あり	Estimated Time of Arrival: December 31
10 mg	$271	在庫あり	Estimated Time of Arrival: December 31
25 mg	$480	在庫あり	Estimated Time of Arrival: December 31
50 mg	$768	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1220	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of AZD5153 6-Hydroxy-2-naphthoic acid:

AZD5153 在庫あり
AZD5153 6-Hydroxy-2-naphthoic acid (Standard) お問い合わせ

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC50: 1.7 nM (BRD4)^[1]

体外実験

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].

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

体内実験

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].

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

臨床実験

分子量

667.75

分子式

C₃₆H₄₁N₇O₆

CAS 番号

1869912-40-2

Appearance

Solid

Color

White to off-white

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (149.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.51%

Select Batch:

データシート (276 KB) SDS (761 KB)

COA (252 KB) HNMR (177 KB) LCMS (98 KB)

取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

動物実験
^[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4976 mL	7.4878 mL	14.9757 mL	37.4392 mL
	5 mM	0.2995 mL	1.4976 mL	2.9951 mL	7.4878 mL
	10 mM	0.1498 mL	0.7488 mL	1.4976 mL	3.7439 mL
	15 mM	0.0998 mL	0.4992 mL	0.9984 mL	2.4959 mL
	20 mM	0.0749 mL	0.3744 mL	0.7488 mL	1.8720 mL
	25 mM	0.0599 mL	0.2995 mL	0.5990 mL	1.4976 mL
	30 mM	0.0499 mL	0.2496 mL	0.4992 mL	1.2480 mL
	40 mM	0.0374 mL	0.1872 mL	0.3744 mL	0.9360 mL
	50 mM	0.0300 mL	0.1498 mL	0.2995 mL	0.7488 mL
	60 mM	0.0250 mL	0.1248 mL	0.2496 mL	0.6240 mL
	80 mM	0.0187 mL	0.0936 mL	0.1872 mL	0.4680 mL
	100 mM	0.0150 mL	0.0749 mL	0.1498 mL	0.3744 mL