Cat. No.: HY-136270

Gartisertib

(Synonyms: VX-803; M4344; ATR inhibitor 2)

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a K_i 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

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Gartisertib Chemical Structure

CAS No.: 1613191-99-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

ATR

<150 pM (Ki)

All ATM/ATR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
LoVo	IC₅₀	86 nM Compound: 5; M4344	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	[PMID: 38299539]
LoVo	IC₅₀	86 nM Compound: M4344; VX-803	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	[PMID: 38955347]

In Vivo

In monotherapy efficacy studies Gartisertib shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression could be observed in triple-negative breast cancer xenograft models^[1].

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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1613191-99-3
Appearance Solid
Molecular Weight 541.55
Formula C₂₅H₂₉F₂N₉O₃
Color Light yellow to yellow
SMILES

O=C(C1=C2N=CC(F)=CN2N=C1N)NC3=C(N4CCC(C(N5CCN(C6COC6)CC5)=O)CC4)C(F)=CN=C3
Synonyms

VX-803; M4344; ATR inhibitor 2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayWBFlow Cytometry

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Journal Impact Factor

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

CHK1 is an integral regulator of DNA replication in human cells. [Abstract]

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.
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.
bioRxiv

RBM39 degrader invigorates natural killer cells to eradicate neuroblastoma despite cancer cell plasticity. [Abstract]

2024 Mar 25:2024.03.21.586157. PMID: 38585889
bioRxiv

2022 Nov 01.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8466 mL

9.2328 mL

18.4655 mL

5 mM

0.3693 mL

1.8466 mL

3.6931 mL

10 mM

0.1847 mL

0.9233 mL

1.8466 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.08 mg/mL (3.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Frank T. Zenke, et al. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Experimental and Molecular Therapeutics.

[2]. Gorecki L, et al. Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacol Ther. 2020 Feb 26:107518. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

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Gartisertib

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Gartisertib

All ATM/ATR Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Gartisertib Related Classifications

HY-136270 Related Classifications