| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Ataxia telangiectasia and Rad3-related (ATR) kinase; functions as a modulator of the DNA damage response (DDR) along with ATM kinase; prevents repair of damaged DNA.
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|---|---|
| ln Vitro |
Elimusertib exhibits potent anti-tumor activity across various lymphoma subtypes, which is associated with replication stress, cell cycle regulation, and CDKN2A loss. It increases efficacy of DNA-damaging cytotoxic therapies.
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| ln Vivo |
In patient-derived xenograft (PDX) models with DDR alterations (21 models tested), elimusertib monotherapy significantly prolonged event-free survival (EFS-2) in 11 models. Partial response or stable disease was observed in models with ATM loss and BRCA1/2 alterations.
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| Enzyme Assay |
ATR kinase activity is measured by gamma-33P-ATP incorporation into a substrate peptide using purified recombinant ATR-ATRIP complex; elimusertib is pre-incubated with the enzyme before adding ATP and substrate; IC50 is determined by scintillation counting.
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| Cell Assay |
Lymphoma cell lines or tumor cells from PDX models are treated with elimusertib (0.1-1000 nM) for 72-120 h; cell viability measured by CellTiter-Glo; DNA damage markers (p-CHK1, gammaH2AX) assessed by Western blot; apoptosis measured by caspase-3/7 activity.
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| Animal Protocol |
PDX models established in immunocompromised mice: elimusertib is administered orally once daily for 21-28 days at doses of 10-50 mg/kg. Tumor volume is measured twice weekly by calipers. Endpoints include event-free survival (time for tumor doubling), partial response, and stable disease.
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| ADME/Pharmacokinetics |
Identical to unlabeled Elimusertib; deuterium labeling does not alter PK properties. Elimusertib is orally bioavailable and exhibits CNS distribution; as an ATR inhibitor, it is used as a radio- and chemosensitizer.
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| Toxicity/Toxicokinetics |
No dedicated toxicity data for the d3 analog. Elimusertib has a manageable safety profile in preclinical studies; common adverse effects include myelosuppression (thrombocytopenia, neutropenia) and gastrointestinal toxicity.
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| References | |
| Additional Infomation |
Elimusertib (BAY 1895344) is an investigational ATR inhibitor under clinical development for treatment of solid tumors and lymphomas; not FDA-approved; the d3-labeled analog is a research-grade analytical standard for LC-MS/MS quantification.
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| Molecular Formula |
C20H18D3N7O
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|---|---|
| Molecular Weight |
378.45
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| Related CAS # |
Elimusertib;1876467-74-1
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| Appearance |
Light yellow to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6424 mL | 13.2118 mL | 26.4236 mL | |
| 5 mM | 0.5285 mL | 2.6424 mL | 5.2847 mL | |
| 10 mM | 0.2642 mL | 1.3212 mL | 2.6424 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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