LY2606368 mesylate
- Prexasertib mesylate
- Parent CAS: 1234015-52-1
- Soluble in DMSO
- MF: C18H19N7O2.CH4O3S
- MW: 461.49
Description
LY2606368 is a potent and selective ATP competitive inhibitor of the CHK protein kinase. It preferentially acts on CHK1 (with a biochemical Ki of 0.9 nM) over CHK2 and RSK (with Ki of 8 nM and 9 nM, respectively). CHK1 is a protein kinase that regulates the tumor cell’s response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, CHK1 blocks cell cycle progression in order to allow to repair damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting CHK1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
More Information
| Parent CAS No. | 1234015-52-1 |
|---|---|
| Chemical Name | 5-(5-(2-(3-Aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile methanesulfonate |
| extra_info | Sold in collaboration with Chemietek |
| MFCD | N.A. |
| Short Description | CHK1 inhibitor |
References
- C King et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13.
- Y Yin et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483.
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