BAY 1895344 (BAY-1895344)
For research use only.
CAS No. 1876467-74-1(freebase)
BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Purity & Quality Control
Choose Selective ATM/ATR Inhibitors
|Description||BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.|
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 hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM).
|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.|
|In vitro||DMSO||82 mg/mL (199.08 mM)|
|Water||82 mg/mL (199.08 mM)|
|Ethanol||82 mg/mL (199.08 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04616534||Not yet recruiting||Drug: Elimusertib|Drug: Gemcitabine||Advanced Fallopian Tube Carcinoma|Advanced Malignant Solid Neoplasm|Advanced Ovarian Carcinoma|Advanced Pancreatic Adenocarcinoma|Advanced Primary Peritoneal Carcinoma|High Grade Ovarian Serous Adenocarcinoma|Platinum-Resistant Fallopian Tube Carcinoma|Platinum-Resistant Ovarian Carcinoma|Platinum-Resistant Primary Peritoneal Carcinoma|Stage II Pancreatic Cancer AJCC v8|Stage IIA Pancreatic Cancer AJCC v8|Stage IIB 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 IIIA Fallopian Tube Cancer AJCC v8|Stage IIIA Ovarian Cancer AJCC v8|Stage IIIA Primary Peritoneal Cancer AJCC v8|Stage IIIA1 Fallopian Tube Cancer AJCC v8|Stage IIIA1 Ovarian Cancer AJCC v8|Stage IIIA2 Fallopian Tube Cancer AJCC v8|Stage IIIA2 Ovarian Cancer AJCC v8|Stage IIIB Fallopian Tube Cancer AJCC v8|Stage IIIB Ovarian Cancer AJCC v8|Stage IIIB Primary Peritoneal Cancer AJCC v8|Stage IIIC Fallopian Tube Cancer AJCC v8|Stage IIIC Ovarian Cancer AJCC v8|Stage IIIC 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|Stage IVA Fallopian Tube Cancer AJCC v8|Stage IVA Ovarian Cancer AJCC v8|Stage IVA Primary Peritoneal Cancer AJCC v8|Stage IVB Fallopian Tube Cancer AJCC v8|Stage IVB Ovarian Cancer AJCC v8|Stage IVB Primary Peritoneal Cancer AJCC v8||National Cancer Institute (NCI)||December 31 2020||Phase 1|
|NCT04267939||Recruiting||Drug: BAY1895344|Drug: Niraparib||Advanced Solid Tumors (Excluding Prostate Cancer)|Ovarian Cancer||Bayer||February 26 2020||Phase 1|
|NCT04095273||Recruiting||Drug: BAY1895344|Drug: Pembrolizumab||Advanced Solid Tumors||Bayer||September 30 2019||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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