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Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名：
LY2606368 mesylate
- 库存：
货期：询盘
- 供应商：
MedChemExpress LLC
- CAS号：
1234015-55-4
- 规格：
询盘
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Prexasertib mesylate
CAS No. : 1234015-55-4
MCE 国际站：Prexasertib mesylate
产品活性：Prexasertib (LY2606368) mesylate 是一种选择性的，ATP 竞争性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂，Ki 为 0.9 nM，IC50 为 <1 nM。Prexasertib mesylate 抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib mesylate 引起双链 DNA 断裂和复制突变，导致细胞凋亡 (apoptosis)。Prexasertib mesylate 显示有效的抗肿瘤活性。
研究领域：Cell Cycle/DNA Damage | Apoptosis
作用靶点：Checkpoint Kinase (Chk) | DNA/RNA Synthesis | Apoptosis
In Vitro: Prexasertib (LY2606368) mesylate inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). Prexasertib mesylate requires CDC25A and CDK2 to cause DNA damage.
Prexasertib mesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells.
Prexasertib mesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells.
Prexasertib mesylate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells.
Prexasertib mesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib mesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA.
In Vivo: Prexasertib mesylate (1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts.
Prexasertib mesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8).
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