Elimusertib (BAY 1895344)

製品コード：S9864 純度：99.99%

Elimusertib (BAY-1895344)は、7 nMのIC50を持つ、非常に強力で選択性の高いATR（毛細血管拡張性運動失調症およびRad3関連）阻害剤です。Elimusertibは、中央値78 nMのIC50で、広範囲のヒト腫瘍細胞株の増殖を強力に阻害します。

CAS No. 1876467-74-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 58000	国内在庫あり
100mg	JPY 143500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（13）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Elimusertib (BAY 1895344)関連製品

関連ターゲット	ATM ATR	もっと見る
関連製品	KU-55933 VE-821 Ceralasertib (AZD6738) KU-60019 Berzosertib (VE-822) AZ20 AZD0156 Mirin AZD1390 CP-466722 Schisandrin B Elimusertib (BAY-1895344) hydrochloride ETP-46464 Gartisertib (M4344, VX-803) CGK 733 AZ31 Lartesertib (M4076) AZ32 HAMNO Cinobufagin ATR Antibody (Rabbit mAb) [P23D7]	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

ATM/ATRシグナル伝達経路

ATM/ATR阻害剤の選択性比較

生物活性

製品説明

Targets

ATR
(Cell-free assay)

7 nM

In Vitro
In vitro	Elimusertib (BAY-1895344) inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines.
細胞実験	細胞株	HT-29 cells, M059J cells, 38 cancer cell lines
	濃度	3–300 nM
	反応時間	72 to 96 hours
	実験の流れ	The antiproliferative activity of Elimusertib (BAY-1895344) is evaluated against a panel of 38 cancer cell lines. After 72 to 96 hours of exposure to this compound, cell proliferation is measured. Cell viability is determined using crystal violet staining or the CellTiter-Glo Cell Viability Assay.

In Vivo
In Vivo	In cancer xenograft models with DNA damage repair deficiencies, Elimusertib (BAY-1895344) exhibits strong monotherapy efficacy.
動物実験	動物モデル	female SCID beige mice, female C.B-17 SCID mice, male NMRI nude mice, female NMRI nude mice
	投与量	50 mg/kg
	投与経路	Oral gavage

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2026-07-31)
NCT04491942	ACTIVE_NOT_RECRUITING	Advanced Bile Duct Carcinoma; Advanced Breast Carcinoma; Advanced Cervical Carcinoma; Advanced Endometrial Carcinoma; Advanced Esophageal Carcinoma; Advanced Gastric Carcinoma; Advanced Head and Neck Carcinoma; Advanced Lung Non-Small Cell Carcinoma; Advanced Lung Small Cell Carcinoma; Advanced Malignant Solid Neoplasm; Advanced Ovarian Carcinoma; Advanced Penile Carcinoma; Advanced Pleural Malignant Mesothelioma; Advanced Urothelial Carcinoma; Anatomic Stage III Breast Cancer AJCC v8; Anatomic Stage IV Breast Cancer AJCC v8; Clinical Stage III Gastric Cancer AJCC v8; Clinical Stage IV Gastric Cancer AJCC v8; Stage III Cervical Cancer AJCC v8; Stage III Distal Bile Duct Cancer AJCC v8; Stage III Intrahepatic Bile Duct Cancer AJCC v8; Stage III Lung Cancer AJCC v8; Stage III Ovarian Cancer AJCC v8; Stage III Penile Cancer AJCC v8; Stage III Pleural Diffuse Malignant Mesothelioma AJCC v8; Stage IV Cervical Cancer AJCC v8; Stage IV Distal Bile Duct Cancer AJCC v8; Stage IV Intrahepatic Bile Duct Cancer AJCC v8; Stage IV Lung Cancer AJCC v8; Stage IV Ovarian Cancer AJCC v8; Stage IV Penile Cancer AJCC v8; Stage IV Pleural Diffuse Malignant Mesothelioma AJCC v8; Triple-Negative Breast Carcinoma; Unresectable Urothelial Carcinoma	National Cancer Institute (NCI)	2021-08-25	PHASE1
NCT04576091	ACTIVE_NOT_RECRUITING	Clinical Stage III HPV-Mediated (p16-Positive) Oropharyngeal Carcinoma AJCC v8; Clinical Stage IV HPV-Mediated (p16-Positive) Oropharyngeal Carcinoma AJCC v8; Recurrent Head and Neck Cutaneous Squamous Cell Carcinoma; Recurrent Head and Neck Squamous Cell Carcinoma; Recurrent Hypopharyngeal Squamous Cell Carcinoma; Recurrent Laryngeal Squamous Cell Carcinoma; Recurrent Oral Cavity Squamous Cell Carcinoma; Recurrent Oropharyngeal Squamous Cell Carcinoma; Recurrent Paranasal Sinus Squamous Cell Carcinoma; Recurrent Salivary Gland Carcinoma; Stage III Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8; Stage III Hypopharyngeal Carcinoma AJCC v8; Stage III Laryngeal Cancer AJCC v8; Stage III Lip and Oral Cavity Cancer AJCC v8; Stage III Major Salivary Gland Cancer AJCC v8; Stage III Oropharyngeal (p16-Negative) Carcinoma AJCC v8; Stage III Sinonasal Cancer AJCC v8; Stage IV Head and Neck Cutaneous Squamous Cell Carcinoma AJCC v8; Stage IV Hypopharyngeal Carcinoma AJCC v8; Stage IV Laryngeal Cancer AJCC v8; Stage IV Lip and Oral Cavity Cancer AJCC v8; Stage IV Major Salivary Gland Cancer AJCC v8; Stage IV Oropharyngeal (p16-Negative) Carcinoma AJCC v8; Stage IV Sinonasal Cancer AJCC v8; Unresectable Head and Neck Cutaneous Squamous Cell Carcinoma; Unresectable Head and Neck Squamous Cell Carcinoma; Unresectable Hypopharyngeal Squamous Cell Carcinoma; Unresectable Laryngeal Squamous Cell Carcinoma; Unresectable Oral Cavity Squamous Cell Carcinoma; Unresectable Oropharyngeal Squamous Cell Carcinoma; Unresectable Paranasal Sinus Squamous Cell Carcinoma; Unresectable Salivary Gland Squamous Cell Carcinoma	National Cancer Institute (NCI)	2022-07-06	PHASE1
NCT04616534	ACTIVE_NOT_RECRUITING	Advanced Fallopian Tube Carcinoma; Advanced Malignant Solid Neoplasm; Advanced Ovarian Carcinoma; Advanced Pancreatic Adenocarcinoma; Advanced Primary Peritoneal Carcinoma; Fallopian Tube High Grade Serous Adenocarcinoma; Metastatic Pancreatic Adenocarcinoma; Ovarian High Grade Serous Adenocarcinoma; Platinum-Resistant Fallopian Tube Carcinoma; Platinum-Resistant Ovarian Carcinoma; Platinum-Resistant Primary Peritoneal Carcinoma; Primary Peritoneal High Grade Serous Adenocarcinoma; Stage II Pancreatic Cancer AJCC v8; Stage III Fallopian Tube Cancer AJCC v8; Stage III Ovarian Cancer AJCC v8; Stage III Pancreatic Cancer AJCC v8; Stage III Primary Peritoneal Cancer AJCC v8; Stage IV Fallopian Tube Cancer AJCC v8; Stage IV Ovarian Cancer AJCC v8; Stage IV Pancreatic Cancer AJCC v8; Stage IV Primary Peritoneal Cancer AJCC v8; Unresectable Pancreatic Adenocarcinoma	National Cancer Institute (NCI)	2021-06-01	PHASE1
NCT04535401	ACTIVE_NOT_RECRUITING	Advanced Colorectal Carcinoma; Advanced Digestive System Carcinoma; Advanced Gastric Carcinoma; Advanced Gastroesophageal Junction Adenocarcinoma; Clinical Stage III Gastric Cancer AJCC v8; Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8; Clinical Stage IV Gastric Cancer AJCC v8; Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8; Metastatic Colorectal Carcinoma; Metastatic Digestive System Carcinoma; Metastatic Gastric Carcinoma; Metastatic Gastroesophageal Junction Adenocarcinoma; Stage III Colorectal Cancer AJCC v8; Stage IV Colorectal Cancer AJCC v8	National Cancer Institute (NCI)	2021-08-13	PHASE1
NCT04514497	ACTIVE_NOT_RECRUITING	Metastatic Lung Small Cell Carcinoma; Metastatic Malignant Solid Neoplasm; Metastatic Neuroendocrine Carcinoma; Metastatic Pancreatic Adenocarcinoma; Stage III Lung Cancer AJCC v8; Stage III Pancreatic Cancer AJCC v8; Stage IV Lung Cancer AJCC v8; Stage IV Pancreatic Cancer AJCC v8; Unresectable Lung Small Cell Carcinoma; Unresectable Malignant Solid Neoplasm; Unresectable Neuroendocrine Carcinoma; Unresectable Pancreatic Adenocarcinoma	National Cancer Institute (NCI)	2021-10-20	PHASE1
NCT05071209	ACTIVE_NOT_RECRUITING	Recurrent Alveolar Rhabdomyosarcoma; Recurrent Ewing Sarcoma; Recurrent Lymphoma; Recurrent Malignant Solid Neoplasm; Refractory Alveolar Rhabdomyosarcoma; Refractory Ewing Sarcoma; Refractory Lymphoma; Refractory Malignant Solid Neoplasm	National Cancer Institute (NCI)	2021-12-22	PHASE1; PHASE2

参考
https://cancerres.aacrjournals.org/content/77/13_Supplement/983 https://pubmed.ncbi.nlm.nih.gov/31582533/

参考

https://cancerres.aacrjournals.org/content/77/13_Supplement/983
https://pubmed.ncbi.nlm.nih.gov/31582533/

化学情報

分子量	375.43	化学式	C₂₀H₂₁N₇O
CAS No.	1876467-74-1	SDF	--
Smiles	CC1COCCN1C2=CC(=C3C=CN=C(C4=CC=N[NH]4)C3=N2)C5=CC=N[N]5C
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 17 mg/mL ( (45.28 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 3 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

* 大学・企業名 大学・企業名を記入してください

* 名前 名前を記入してください

* 電子メール 電子メール・アドレスを記入してください 有効なメールアドレスを入力してください

電話番号

* 内容 お問い合わせ内容をご入力ください

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):