LY 2603618

Pricing Availability   Qty
Cat.No. 6454 - LY 2603618 | C18H22BrN5O3 | CAS No. 911222-45-2
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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).

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.73 20

Preparing Stock Solutions

The following data is based on the product molecular weight 436.3. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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 pemetrexed and cisplatin in patients with advanced cancer. Invest.New Drugs 32 955 PMID: 24942404


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Literature in this Area

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Cancer

Cancer Research Product Guide

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Cell Cycle & DNA Damage Repair

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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.