Ceralasertib (Synonyms: AZD6738)

Name: Ceralasertib
Brand: MedChemExpress
SKU: HY-19323
Rating: 5.0 (60 reviews)

製品番号: HY-19323 純度: 99.43%: Data Sheet SDS COA 取扱説明書
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Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC₅₀ of 1 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。

CAS 番号 : 1352226-88-0

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$120	在庫あり	Estimated Time of Arrival: December 31
10 mg	$180	在庫あり	Estimated Time of Arrival: December 31
25 mg	$330	在庫あり	Estimated Time of Arrival: December 31
50 mg	$528	在庫あり	Estimated Time of Arrival: December 31
100 mg	$888	在庫あり	Estimated Time of Arrival: December 31
500 mg	$2100	在庫あり	Estimated Time of Arrival: December 31
1 g	$2950	在庫あり	Estimated Time of Arrival: December 31
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10 g		お問い合わせ

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* 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 60 publication(s) in Google Scholar

Other Forms of Ceralasertib:

(S)-Ceralasertib 在庫あり
Ceralasertib formate お問い合わせ

顧客検証

In Vivo Efficacy Study

: Ceralasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 16;15(1):1446. [Abstract]; Immunoblot of KPC cells harboring doxycycline-inducible shRNA targeting luciferase, components of the PAF1c and MYC. Depletion was induced by doxycycline addition for 72 h and AZD6738 treatment for 72 h at 0.2 µM concentration. * refers to a non-specific band. Beta-actin was loading control (n=3).

: Ceralasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 16;15(1):1446. [Abstract]; pKAP1(S824) intensity upon incubation with AZD6738 (0.1 µM; 24 h) (number of KPC cells plotted: siNTC: n=1654; siCDC73:n=1175).Scale bar: 10 µm. siRNA transfection was 48 h and EdU was added 30 minutes before fixation.

: Ceralasertib purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 Jan 11;52(1):204-222. [Abstract]; AZD6738 (1 μM) were administered for 30 minutes prior to UV irradiation (20 J/m²). HeLa cells were allowed to recover for 2 h after UV treatment, and phosphorylation of DHX9, Chk1, Chk2, and RPA32 was assessed by Western blot with indicated antibodies.

: Ceralasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Aug 4;13(1):4520. [Abstract]; ATR inhibitor AZD6738 prevent NCI‐H929 TP53^−/− cell growth in NSG mice. NSG mice were subcutaneously injected with 10⁶ NCI‐H929 TP53^−/− cells (left panel). After 1 week, mice with detectable tumors were randomly distributed into four groups of seven mice and treated with AZD6738 (25 mg/kg; i.g., 5 times a week for 2 weeks), as indicated by the arrows (middle panel). The graphs represent the tumor volume kinetics (mean±SD, middle panel) and the tumor volume on Day 12 (right panel).

: Ceralasertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Nov 16;41(1):323. [Abstract]; Ceralasertib (AZD6738; 1, 2 µM) signifcantly decreases the protein levels of ATR, IFI16 and HuR in a dose-dependent manner in GSC 267 and GSC 20 cells.

ATM/ATR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

ATM ATR TRRAP

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製品説明

Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC₅₀ of 1 nM.

IC₅₀ & Target^[1]

ATR

1 nM (IC₅₀)

PI3Kδ

6.8 μM (IC₅₀)

DYRK

10.8 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.62 μM Compound: 5; AZD6738	Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
A549	IC₅₀	2 μM Compound: AZD6738	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 35191694]
CAPAN-1	IC₅₀	5.54 μM Compound: 5; AZD6738	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
DLD-1	IC₅₀	5.28 μM Compound: 5; AZD6738	Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
Granta-519	IC₅₀	0.55 μM Compound: 5; AZD6738	Antiproliferative activity against human Granta-519 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Granta-519 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
HCT-116	IC₅₀	1.12 μM Compound: 5; AZD6738	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
HCT-116	IC₅₀	3.62 μM Compound: AZD6738	Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay	[PMID: 38325007]
HT-29	GI₅₀	2.6 μM Compound: 2; AZD6738	Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 30346772]
HT-29	IC₅₀	2.59 μM Compound: 5; AZD6738	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
LoVo	GI₅₀	0.44 μM Compound: 2; AZD6738	Cytotoxicity against human LoVo cells after 72 hrs by MTS assay Cytotoxicity against human LoVo cells after 72 hrs by MTS assay	[PMID: 30346772]
LoVo	IC₅₀	0.83 μM Compound: AZD6738	Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay	[PMID: 38325007]
LoVo	IC₅₀	1.14 μM Compound: 5; AZD6738	Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
LoVo	IC₅₀	377 nM Compound: 2	Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay	[PMID: 38299539]
NCI-H446	IC₅₀	1.96 μM Compound: 5; AZD6738	Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
OCI-Ly10	IC₅₀	0.52 μM Compound: 5; AZD6738	Antiproliferative activity against human OCI-Ly10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human OCI-Ly10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
PC-3	IC₅₀	11.28 μM Compound: 5; AZD6738	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]
SUD4	IC₅₀	2.26 μM Compound: 5; AZD6738	Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 39053006]

体外実験

Ceralasertib (AZD6738) is a potent inhibitor of ATR kinase activity with an IC₅₀ of 0.001 μM against the isolated enzyme and 0.074 μM against ATR kinase-dependent CHK1 phosphorylation in cells. Ceralasertib (AZD6738) induces cell death and senescence in non-small cell lung cancer (NSCLC) cell lines. Ceralasertib (AZD6738) impairs viability of four Kras mutant cell lines: H23, H460, A549, and H358. , with the lowest GI₅₀ and greatest maximal inhibition in H460 and H23 cells (1.05 μM, 88.0% and 2.38 μM, 86.2%, respectively). Ceralasertib (AZD6738) potentiates the cytotoxicity of CDDP and NSC 613327 in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with CDDP in ATM-deficient NSCLC cells^[1]. Ceralasertib (AZD6738) inhibits human breast cancer cell lines with IC₅₀ values less than 1 μM using MTT assay. Ceralasertib (AZD6738) induces cell cycle arrest and apoptosis. It downregulates DNA damage response molecules and cell proliferative signaling molecules^[2].

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

体内実験

Daily administration of Ceralasertib (AZD6738) and ATR kinase inhibition for 14 consecutive days is tolerated in mice and enhances the therapeutic efficacy of CDDP in xenograft models. Remarkably, the combination of CDDP and Ceralasertib (AZD6738) resolves ATM-deficient lung cancer xenografts^[1].

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

臨床実験

分子量

412.51

分子式

C₂₀H₂₄N₆O₂S

CAS 番号

1352226-88-0

Appearance

Solid

Color

Off-white to light brown

SMILES

O=[S@@](C1(CC1)C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(N5CCOC[C@H]5C)=C2)(C)=N

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 70 mg/mL (169.69 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	2.4242 mL	12.1209 mL	24.2418 mL
5 mM	0.4848 mL	2.4242 mL	4.8484 mL
10 mM	0.2424 mL	1.2121 mL	2.4242 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. 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: ≥ 5 mg/mL (12.12 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 2.08 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (24.24 mM); Clear solution; Need ultrasonic

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).

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: 99.76%

Select Batch:

データシート (281 KB) SDS (557 KB)

COA (253 KB) HNMR (194 KB) LCMS (467 KB) Elemental Analysis Report (111 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo. [Content Brief]

[2]. Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119. [Content Brief]

細胞実験 ^[1]	Ceralasertib (AZD6738) is dissolved in DMSO at 30 mM and diluted in DMSO to desired working concentrations. The final DMSO concentration in media for all conditions and controls is 0.1% for Ceralasertib (AZD6738) dose response experiments, 0.05% for Ceralasertib (AZD6738) + chemotherapy viability experiments, and 0.025% for all experiments involving 0.3 μM and 1.0 μM doses of Ceralasertib (AZD6738)^[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。
動物実験 ^[1]	Mice^[1] Ceralasertib (AZD6738) is dissolved in DMSO at a concentration of 25 mg/mL or 50 mg/mL and diluted 1:5 in propylene glycol. Ceralasertib (AZD6738) is administered by oral gavage at 25 mg/kg (H23) or 50 mg/kg (H460) for 14 consecutive days. The dosing volume is 10 mL/kg.^[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]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo. [Content Brief] [2]. Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4242 mL	12.1209 mL	24.2418 mL	60.6046 mL
	5 mM	0.4848 mL	2.4242 mL	4.8484 mL	12.1209 mL
	10 mM	0.2424 mL	1.2121 mL	2.4242 mL	6.0605 mL
	15 mM	0.1616 mL	0.8081 mL	1.6161 mL	4.0403 mL
	20 mM	0.1212 mL	0.6060 mL	1.2121 mL	3.0302 mL
	25 mM	0.0970 mL	0.4848 mL	0.9697 mL	2.4242 mL
	30 mM	0.0808 mL	0.4040 mL	0.8081 mL	2.0202 mL
	40 mM	0.0606 mL	0.3030 mL	0.6060 mL	1.5151 mL
	50 mM	0.0485 mL	0.2424 mL	0.4848 mL	1.2121 mL
	60 mM	0.0404 mL	0.2020 mL	0.4040 mL	1.0101 mL
	80 mM	0.0303 mL	0.1515 mL	0.3030 mL	0.7576 mL
	100 mM	0.0242 mL	0.1212 mL	0.2424 mL	0.6060 mL

Ceralasertib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ceralasertib1352226-88-0AZD6738AZD 6738AZD-6738ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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Ceralasertib (Synonyms: AZD6738)

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ATM/ATR アイソフォーム固有の製品をすべて表示:

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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

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ceralasertib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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Ceralasertib (Synonyms: AZD6738)

カスタマーレビュー

Other Forms of Ceralasertib:

Ceralasertib 関連抗体

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:

ATM/ATR アイソフォーム固有の製品をすべて表示:

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

Ceralasertib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ceralasertib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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Request for HNMR Report

Request for HNMR Report