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| Targets |
Lartesertib targets ataxia-telangiectasia mutated (ATM) kinase, a serine/threonine protein kinase that plays a critical role in the DNA damage response (DDR) pathway. ATM is activated by DNA double-strand breaks and phosphorylates downstream targets involved in cell cycle checkpoint activation, DNA repair, and apoptosis. By inhibiting ATM kinase activity in an ATP-competitive manner, Lartesertib disrupts the DDR pathway, sensitizing cancer cells to DNA-damaging agents such as chemotherapy and radiotherapy.
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| ln Vitro |
In vitro, Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. It can inhibit the growth of multiple hematopoietic cell lines. The compound has potential anticancer activity. Specific in vitro data such as IC50 values are not detailed in the available literature, but the compound is characterized as a high-potency ATM inhibitor.
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| ln Vivo |
In vivo, Lartesertib is orally bioavailable. Upon oral administration, it targets and binds to ATM, inhibiting its kinase activity and its mediated signaling pathways. The compound has potential chemo-sensitizing/radiotherapy-enhancing and antitumor activities. It can be used for the study of lung cancer.
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| Enzyme Assay |
In vitro kinase assays are used to characterize Lartesertib's inhibition of ATM kinase. ATM is incubated with varying concentrations of the compound and ATP substrate. Kinase activity is measured by phosphorylation of a peptide substrate. Inhibition is determined from dose-response curves. The compound is an ATP-competitive inhibitor.
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| Cell Assay |
Cell-based assays for Lartesertib are conducted in cancer cell lines. Cells are treated with the compound, and ATM kinase activity is assessed by measuring the phosphorylation of ATM substrates such as p53 and CHK2. Cell viability and apoptosis are also assessed. These assays confirm the compound's ability to inhibit ATM signaling and its anti-proliferative effects.
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| Animal Protocol |
In vivo animal experiments with Lartesertib are conducted in xenograft models. The compound is administered orally, and tumor growth inhibition is assessed. The compound's ability to sensitize tumors to chemotherapy or radiotherapy is also evaluated. Specific protocols are not extensively documented.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lartesertib include oral bioavailability. The compound has a molecular formula of C23H21FN6O3 and a molecular weight of 448.45. Solubility: DMSO: ≥90 mg/mL. Appearance: Solid. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for Lartesertib are limited. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. No specific toxicity data are available.
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| References | |
| Additional Infomation |
Lartesertib is an orally bioavailable ATP-competitive ataxia-telangiectasia mutant kinase (ATM) inhibitor with potential chemosensitizing/radiotherapy-enhancing and antitumor activities. After oral administration, lartesertib targets and binds to ATM, thereby inhibiting ATM kinase activity and its mediated signaling pathways. This prevents activation of DNA damage checkpoints, interferes with DNA damage repair, induces tumor cell apoptosis, and leads to the death of ATM-overexpressing tumor cells. Furthermore, by inhibiting DNA damage repair, M4076 enhances the sensitivity of tumor cells to chemotherapy and radiotherapy and improves their antitumor activity. ATM is a serine/threonine protein kinase upregulated in various cancer cell types; it is activated after DNA damage and plays a crucial role in DNA chain repair.
Lartesertib has CAS number 2495096-26-7, molecular formula C23H21FN6O3, and molecular weight 448.45. Synonyms: ATM Inhibitor-5, M4076. It is an orally bioavailable ATP-competitive ATM kinase inhibitor with potential anticancer activity. Purity: 99.94%. Not for human use; for research purposes only. |
| Molecular Formula |
C23H21FN6O3
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|---|---|
| Molecular Weight |
448.45
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| Exact Mass |
448.166
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| CAS # |
2495096-26-7
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| Related CAS # |
(Rac)-Lartesertib;2020089-41-0
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| PubChem CID |
122599280
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
732
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C(N(C2=C(F)C=NC=C2OC)C2C1=CN=C1C=2C=C(C(=C1)OC)C1C(C)=NN(C=1)C)=O)C
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| InChi Key |
WNEFOSMCGCLLJU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21FN6O3/c1-12-15(11-28(2)27-12)13-6-14-17(7-19(13)32-4)26-9-18-21(14)30(23(31)29(18)3)22-16(24)8-25-10-20(22)33-5/h6-11H,1-5H3
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| Chemical Name |
IUPAC Name:
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| Synonyms |
Lartesertib; M-4076; M4076; M 4076; 8-(1,3-Dimethyl-1H-pyrazol-4-yl)-1-(3-fluoro-5-methoxy-4-pyridinyl)-1,3-dihydro-7-methoxy-3-methyl-2H-imidazo(4,5-C)quinolin-2-one; compound 1M [PMID: 34662544]; 2H-Imidazo(4,5-C)quinolin-2-one, 8-(1,3-dimethyl-1H-pyrazol-4-yl)-1-(3-fluoro-5-methoxy-4-pyridinyl)-1,3-dihydro-7-methoxy-3-methyl-;
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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) |
DMSO : ≥ 100 mg/mL (~223.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2299 mL | 11.1495 mL | 22.2990 mL | |
| 5 mM | 0.4460 mL | 2.2299 mL | 4.4598 mL | |
| 10 mM | 0.2230 mL | 1.1150 mL | 2.2299 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05396833
Conditions:Metastatic or Locally Advanced Unresectable Solid TumorsLink: https://clinicaltrials.gov/ct2/show/NCT06433219
Conditions:Ovarian CancerLink: https://clinicaltrials.gov/ct2/show/NCT04882917
Conditions:Advanced Solid TumorsProducts are for research use only; We do not sell to patients
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