| Field | Specification |
|---|---|
| Target | |
| Alternative names | M4076; ATM Inhibitor-5 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C23H21FN6O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Lartesertib, also known as M4076 or ATM Inhibitor-5, is a highly potent inhibitor of the serine/threonine protein kinase ATM. It can inhibit the growth of multiple hematopoietic cell lines, and when combined with the ATR inhibitor tuvusertib it can promote tumor cell death, activate the immune signaling pathway, and exhibit anti-tumor activity[1][2]. It is supplied as a white to off-white solid (C23H21FN6O3, MW 448.45) at 99.94% purity.
Physical & Chemical Properties
| CAS Number | 2495096-26-7 |
|---|---|
| Molecular Formula | C23H21FN6O3 |
| Molecular Weight | 448.45 g/mol |
| Purity | 99.94% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(N1C2=C(F)C=NC=C2OC)N(C)C3=C1C4=CC(C5=CN(C)N=C5C)=C(OC)C=C4N=C3 |
| Target | ATM |
| Signaling Pathway | Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Immunology/Inflammation |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (222.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
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]. Mukker J K, et al. In vitro evaluation of myelosuppressive effects of ATRi tuvusertib and ATMi lartesertib (M4076), alone and in combination. Cancer Research, 2024, 84(6_Supplement): 7186-7186.
[2]. Laaber K, et al. Combined inhibition of ATR and ATM with tuvusertib and lartesertib (M4076) impacts the tumor microenvironment. Cancer Research, 2024, 84(6_Supplement): 5617-5617.
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 | ≥ 100 mg/mL (222.99 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); 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 + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.57 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.57 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 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 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.57 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Lartesertib (0.01-10 μM; 3-7 days) may inhibit erythroid, megakaryocytic and myeloid hematopoietic cells within peripheral blood CD34+ cells[1]. Together with Tuvusertib, Lartesertib can cause MC-38 cell death, activate the STING signaling pathway, upregulate PD-L1, and release inflammatory cytokines[2].
In Vivo
In the MC-38 mouse tumor model, Lartesertib can change the tumor microenvironment. Treatment for 24 to 72 hours significantly upregulates PD-L1 on immune cells and tumor cells. With prolonged treatment (23 days), PD-L1 expression and the tumor immune cell population change: PD-L1 remains expressed on tumor cells but at a significantly reduced level, CD8+ T cells are depleted, and NK cells increase significantly[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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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
AURKA inhibitor VIC-1911 induces mitotic defects and functional BRCAness, sensitizing prostate cancer to PARP inhibition. JCI Insight 2026 Mar 31:e196665. PMID: 41915443
Molecular Characterization of PARP Inhibitor Response Reveals Co-Targeting Strategies in Advanced Prostate Cancer. Cancers (Basel) 2026 Jul 23;18(15):2381. PMID: 42588601
Biomedicines. 2026 May;14(5):949.
