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Prexasertib dimesylate

CAS No. : 1234015-58-7

MCE 国际站：Prexasertib dimesylate

产品活性：Prexasertib dimesylate (LY2606368 dimesylate) 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，K_i 为 0.9 nM，IC₅₀ 为 <1 nM。Prexasertib dimesylate 抑制 CHK2 (IC₅₀=8 nM) 和 RSK1 (IC₅₀=9 nM)。Prexasertib dimesylate 引起双链 DNA 断裂和复制突变，导致细胞凋亡 (apoptosis)。Prexasertib dimesylate 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)  |  Apoptosis

In Vitro: Prexasertib dimesylate (LY2606368 dimesylate) inhibits MELK (IC₅₀=38 nM), SIK (IC₅₀=42 nM), BRSK2 (IC₅₀=48 nM), ARK5 (IC₅₀=64 nM). Prexasertib dimesylate requires CDC25A and CDK2 to cause DNA damage.
Prexasertib dimesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells.
Prexasertib dimesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells.
Prexasertib dimesylate (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 dimesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib dimesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA.

In Vivo: Prexasertib dimesylate (LY2606368 dimesylate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts.
Prexasertib dimesylate (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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