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编 号：F084921
分子式：C19H23N7O5S
分子量：461.49
分子式：C19H23N7O5S
分子量：461.49
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CAS No: 1234015-55-4
产品详情
生物活性：
Prexasertib mesylate (LY2606368 mesylate) 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 mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.
体内研究：
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).Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells
Dosage:1, 3.3, or 10 mg/kg
Administration:SC; twice daily for 3 days, rest 4 days; for three cycles
Result:Caused statistically significant tumor growth inhibition (up to 72.3%).
体外研究：
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.
Prexasertib mesylate (LY2606368 mesylate) 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 mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.
体内研究：
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).Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells
Dosage:1, 3.3, or 10 mg/kg
Administration:SC; twice daily for 3 days, rest 4 days; for three cycles
Result:Caused statistically significant tumor growth inhibition (up to 72.3%).
体外研究：
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.
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