Elimusertib (BAY-1895344) hydrochloride

別名：BAY-1895344 HCl

製品コード：S8666 純度：99.09%

Elimusertib (BAY-1895344) hydrochlorideは、IC50が7 nMの強力で選択性の高い経口投与可能なATR阻害剤です。

Elimusertib (BAY-1895344) hydrochloride化学構造

CAS No.

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 43300	国内在庫あり
2mg	JPY 22000	国内在庫あり
5mg	JPY 40500	国内在庫あり
25mg	JPY 85500	国内在庫あり
100mg	JPY 205500	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（11）

製品安全説明書

現在のバッチを見る：純度： 99.09%

99.09

Elimusertib (BAY-1895344) hydrochloride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 Elimusertib (BAY 1895344) CP-466722 Schisandrin B 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	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle 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

Elimusertib (BAY-1895344) hydrochlorideは、IC50が7 nMの強力で選択性の高い経口投与可能なATR阻害剤です。

Targets

ATR
(Cell-free assay)

7 nM

In Vitro
In vitro	In vitro, BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits induced H2AX phosphorylation (IC50 = 36 nM).
細胞実験	細胞株	C4–2b and PC-3 cells
	濃度	2 μM
	反応時間	48 h
	実験の流れ	Cells were treated with various concentrations of BAY1895344.

In Vivo
In Vivo	BAY 1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models.
動物実験	動物モデル	C57BL/6N male mice
	投与量	40 mg/kg
	投与経路	i.p.

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
http://cancerres.aacrjournals.org/content/77/13_Supplement/983 http://cancerres.aacrjournals.org/content/77/13_Supplement/836 https://pubmed.ncbi.nlm.nih.gov/34168048/

参考

http://cancerres.aacrjournals.org/content/77/13_Supplement/983
http://cancerres.aacrjournals.org/content/77/13_Supplement/836
https://pubmed.ncbi.nlm.nih.gov/34168048/

化学情報

分子量	411.89	化学式	C₂₀H₂₂ClN₇O
CAS No.		SDF	Download Elimusertib (BAY-1895344) hydrochloride SDFをダウンロードする
Smiles	CC1COCCN1C2=NC3=C(C=CN=C3C4=CC=NN4)C(=C2)C5=CC=NN5C
保管	3年-20°C粉	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年-20°C粉	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 : 82 mg/mL ( (199.08 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。)

Water : 82 mg/mL

Ethanol : 82 mg/mL

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
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (2.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.250mg/ml (0.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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。

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