2781996-46-9
Chemical Structure
Prexasertib lactate
Synonym(s): LY2606368 lactate
- CAS No.: 2781996-46-9
- Formula:C21H25N7O5
- Molecular Weight:455.47
InChIKey: BQURYWIMQXBZFL-WNQIDUERSA-N
SMILES: OC([C@@H](O)C)=O.NCCCOC1=C(C2=CC(NC3=NC=C(C#N)N=C3)=NN2)C(OC)=CC=C1
Biological Activity: Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity[1][2].
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Prexasertib lactate | Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity. | |||||||||||||||||||||
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References
- [1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1 [Content Brief]
- [2]. Yin Y, 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. [Content Brief]
