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Description: Potent and selective Chk1 inhibitor
Chemical Name: N-[5-Bromo-4-methyl-2-[(2S)-2-morpholinylmethoxy)phenyl]-N'-(5-methyl-2-pyrazinyl)urea
Purity: ≥98% (HPLC)
Biological Activity for LY 2603618
LY 2603618 is a potent and selective Chk1 inhibitor (IC50 = 7 nM). Inhibits Chk1 autophosphorylation. Induces cell cycle arrest in the G2/M phase and induces the DNA damage response in lung cancer cells. Inhibits growth of NSCLC xenografts in mice when administered in combination with Pemetrexed (Cat.No. 6185).
Compound Libraries for LY 2603618
LY 2603618 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 2603618
| M. Wt | 436.3 |
| Formula | C18H22BrN5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 911222-45-2 |
| PubChem ID | 11955855 |
| InChI Key | SYYBDNPGDKKJDU-ZDUSSCGKSA-N |
| Smiles | CC1=CN=C(C=N1)NC(NC2=C(C=C(C(Br)=C2)C)OC[C@@H]3CNCCO3)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LY 2603618
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.73 | 20 |
Preparing Stock Solutions for LY 2603618
The following data is based on the product molecular weight 436.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 11.46 mL | 57.3 mL | 114.6 mL |
| 1 mM | 2.29 mL | 11.46 mL | 22.92 mL |
| 2 mM | 1.15 mL | 5.73 mL | 11.46 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.29 mL |
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Product Datasheets for LY 2603618
References for LY 2603618
References are publications that support the biological activity of the product.
Wang et al (2014) The checkpoint 1 kinase inhibitor LY2603618 induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Apoptosis 19 1389 PMID: 24928205
Calvo et al (2014) Preclinical analyses and phase I evaluation of LY2603618 administered in combination with pemet. and cisp. in patients with advanced cancer. Invest.New Drugs 32 955 PMID: 24942404
If you know of a relevant reference for LY 2603618, please let us know.
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Keywords: LY 2603618, LY 2603618 supplier, LY2603618, checkpoint, Chk1, inhibitors, inhibits, potent, selective, DNA, damage, response, cell, cycle, arrest, Checkpoint, Control, Kinases, 6454, Tocris Bioscience
1 Citation for LY 2603618
Citations are publications that use Tocris products. Selected citations for LY 2603618 include:
Adam M et al (2022) Inhibition of Chk2 promotes neuroprotection, axon regeneration, and functional recovery after CNS injury. Sci Adv 8 eabq2611 PMID: 36103534
Do you know of a great paper that uses LY 2603618 from Tocris? Please let us know.
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.