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Medchemexpress LLC Prexasertib (dihydrochloride) | 1234015-54-3 | 99.7% | 438.31 | 50 MG

Supplier: Medchemexpress LLC HY18174A50MG
Prexasertib dihydrochloride is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with potent anti-tumor activity. It causes double-stranded DNA breakage and replication catastrophe, leading to apoptosis.
- Selective CHK1 inhibitor with Ki of 0.9 nM and IC50 of <1 nM
- Also inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM)
- Causes double-stranded DNA breakage
- Induces replication catastrophe and apoptosis
- Demonstrates potent anti-tumor activity
- Inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), and ARK5 (IC50=64 nM)
- Requires CDC25A and CDK2 to induce DNA damage
- Causes chromosomal fragmentation in HeLa cells
- Induces replication stress and depletes RPA2 available for DNA binding
- Shows tumor growth inhibition in xenografts
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