Gartisertib
Based on 6 publication(s) in Google Scholar
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
For research use only. We do not sell to patients.
- Purity : 99.77%
- CAS No.: 1613191-99-3
- Formula: C25H29F2N9O3
- Molecular Weight:541.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gartisertib
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
Biological Activity
Description
IC50 & Target
[1]|
ATR <150 pM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | IC50 |
86 nM
Compound: 5; M4344
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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
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[PMID: 38299539] |
| LoVo | IC50 |
86 nM
Compound: M4344; VX-803
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Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured for 48 hrs byT assay
Antiproliferative activity against human LoVo cells assessed as reduction in cell viability measured for 48 hrs byT assay
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[PMID: 38955347] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1613191-99-3
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Appearance Solid
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Molecular Weight 541.55
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Formula C25H29F2N9O3
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Color Light yellow to yellow
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SMILES
O=C(C1=C2N=CC(F)=CN2N=C1N)NC3=C(N4CCC(C(N5CCN(C6COC6)CC5)=O)CC4)C(F)=CN=C3
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Synonyms
VX-803; M4344; ATR inhibitor 2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Commun
RBM39 degrader invigorates innate immunity to eradicate neuroblastoma despite cancer cell plasticity. [Abstract]2025 Sep 17;16(1):8287. PMID: 40962798 -
Cell Death Dis
2026 Mar 26;17(1):375. PMID: 41888112
Gartisertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
The ATR inhibitor Gartisertib (0.625-32 μM; 24 h) markedly reduced the viability of parental 293A cells.
Gartisertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
Gartisertib (ATRi) (1 μM; 2-24 h) induced DNA damage markers and mitotic entry defects in 293A cells.
Gartisertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
Flow cytometry analysis of EdU incorporation showed that Gartisertib (ATRi) (0.625 μM) caused replication stress and S-phase progression defects in 293A cells.
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EMBO Rep
Tumor acidosis-induced DNA damage response and tetraploidy enhance sensitivity to ATM and ATR inhibitors. [Abstract]2024 Mar;25(3):1469-1489. PMID: 38366255
Gartisertib purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2024 Mar;25(3):1469-1489. [Abstract]
In HCT116 spheroids, Gartisertib (ATRi) (1-30 μM; 72 h) led to a significant growth inhibition when used as a single agent and enhanced the effects of 5-FU when concomitantly administered.
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bioRxiv
RBM39 degrader invigorates natural killer cells to eradicate neuroblastoma despite cancer cell plasticity. [Abstract]2024 Mar 25:2024.03.21.586157. PMID: 38585889 -
Gartisertib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2022 Nov 01.
Gartisertib (ATRi-2) (0.3 μM) nearly tripled the frequency of neotelomere formation in RPE1-ST cells.
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (46.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.84 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8466 mL | 9.2328 mL | 18.4655 mL | 46.1638 mL |
| 5 mM | 0.3693 mL | 1.8466 mL | 3.6931 mL | 9.2328 mL | |
| 10 mM | 0.1847 mL | 0.9233 mL | 1.8466 mL | 4.6164 mL | |
| 15 mM | 0.1231 mL | 0.6155 mL | 1.2310 mL | 3.0776 mL | |
| 20 mM | 0.0923 mL | 0.4616 mL | 0.9233 mL | 2.3082 mL | |
| 25 mM | 0.0739 mL | 0.3693 mL | 0.7386 mL | 1.8466 mL | |
| 30 mM | 0.0616 mL | 0.3078 mL | 0.6155 mL | 1.5388 mL | |
| 40 mM | 0.0462 mL | 0.2308 mL | 0.4616 mL | 1.1541 mL |
Gartisertib Related Classifications
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