Antibodies
LY2603618
- 貨號 Cat. No.
- S2626
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
LY2603618
LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity. | |||||
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| Targets | Chk1 | |||||
| IC50 | ||||||
| In vitro | Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3] | |||||
| In vivo | In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00415636 | Completed | Cancer | Eli Lilly and Company | 2006-12 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 436.3 |
|---|---|
| Formula | C18H22BrN5O3 |
| CAS No. | 911222-45-2 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 13 mg/mL (29 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (S)-1-(5-bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl)-3-(5-methylpyrazin-2-yl)urea |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.4363 | 4.363 | 8.726 | - |
Customer Reviews (2)
 Click to enlarge | Rating | |
| Source | Customer W, F. Z.. LY2603618 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | C6 cell | |
| Concentrations | 1-20 uM | |
| Incubation Time | 24 h | |
| Results | CHK1 phosphorylation increased at 1 and 5uM of LY2603618. At even 20uM, CHK1 phosphorylation was not inhibited. These are possibly due to a strong negative feedback, or to prevention of phosphatase proximity. DNA damage indicator, H2AX phosphorylation, was evident at as low as 1uM. |
Product Citations (3)
Cellular Impedance Assays for Predictive Preclinical Drug Screening of Kinase Inhibitor Cardiovascular Toxicity. [Lamore SD, et al. Toxicol Sci 2013;135(2):402-13]
Panobinostat Synergistically Enhances the Cytotoxic Effects of Cisplatin, Doxorubicin or Etoposide on High-Risk Neuroblastoma Cells [Wang G, et al. PLoS One 2013;8(9):e76662]
PARP and CHK inhibitors interact to cause DNA damage and cell death in mammary carcinoma cells. [Laurence Booth, et al. Cancer Biology & Therapy 2013;14(5):458-65]
