| Field | Specification |
|---|---|
| Target | |
| Alternative names | VX-803; M4344; ATR inhibitor 2 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H29F2N9O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Gartisertib, also known as VX-803, M4344, or ATR inhibitor 2, is an ATP-competitive, orally active, selective ATR inhibitor with a Ki of less than 150 pM. It potently inhibits ATR-driven phosphorylation of checkpoint kinase-1 (Chk1), with an IC50 of 8 nM, and shows antitumor activity[1][2]. It is supplied as a light yellow to yellow solid (C25H29F2N9O3, MW 541.55) at 99.77% purity.
Physical & Chemical Properties
| CAS Number | 1613191-99-3 |
|---|---|
| Molecular Formula | C25H29F2N9O3 |
| Molecular Weight | 541.55 g/mol |
| Purity | 99.77% |
| Appearance | Solid |
| 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 |
| Target | ATR |
| Signaling Pathway | Cell Cycle/DNA Damage; PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: 25 mg/mL (46.16 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
ATR <150 pM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under 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.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (46.16 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (3.84 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | 2.08 mg/mL (3.84 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.08 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
Gartisertib monotherapy produces tumor stasis to regression in efficacy studies of tumor models with alternative lengthening of telomeres (ALT). When combined with PARP inhibitors, Gartisertib leads to tumor regression in triple-negative breast cancer xenograft models[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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RBM39 degrader invigorates innate immunity to eradicate neuroblastoma despite cancer cell plasticity. Nat Commun 2025 Sep 17;16(1):8287. PMID: 40962798
CHK1 is an integral regulator of DNA replication in human cells. Cell Death Dis 2026 Mar 26;17(1):375. PMID: 41888112
LIG1 Loss in TP53-mutant Triple Negative Breast Cancer Rewires DNA Repair and Confers Sensitivity to PARP-ATR Inhibitor Combinations. Mol Cancer Ther 2026 Jul 15:10.1158/1535-7163.MCT-26-0182. PMID: 42456172
Tumor acidosis-induced DNA damage response and tetraploidy enhance sensitivity to ATM and ATR inhibitors. EMBO Rep 2024 Mar;25(3):1469-1489. PMID: 38366255
RBM39 degrader invigorates natural killer cells to eradicate neuroblastoma despite cancer cell plasticity. bioRxiv 2024 Mar 25:2024.03.21.586157. PMID: 38585889
bioRxiv. 2022 Nov 01.
