ly2606368

Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变，导致细胞凋亡。

Prexasertib is a potent and selective Chk1 Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B- T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-d

LY2606368 HCl is a selective ATP competitive inhibitor of checkpoint kinase 1 (IC50: 1.5nM in SW1990 cells).

Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective ATP-competitive second-generation inhibitor of checkpoint kinase 1 (CHK1). With a K i of 0.9 nM and an IC 50 of <1 nM, Prexasertib dimesylate effectively inhibits CHK2 (IC 50 = 8 nM) and RSK1 (IC 50 = 9 nM). Its mechanism of action involves inducing double-stranded DNA breakage and replication catastrophe, ultimately leading to apoptosis. Moreover, Prexasertib dimesylate demonstrates potent anti-tumor activity.

Prexasertib is an effective and selective Chk1 Chk2 inhibitor. Prexasertib causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms.

Prexasertib dihydrochloride (LY2606368) 是一种选择性的，ATP 竞争性的细胞周期检测点激酶 1 抑制剂，Ki 为 0.9 nM，IC50为 <1 nM。它抑制 CHK2(IC50=8 nM) 和 RSK1 (IC50=9 nM)。它引起双链 DNA 断裂和复制突变，导致细胞凋亡，有抗肿瘤活性。

Prexasertib lactate 是 Prexasertib 的乳酸盐形式，这种化合物是选择性的 ATP 竞争性第二代细胞周期检测点激酶 1 (CHK1) 抑制剂，具有 Ki 值为 0.9 nM 和 IC50 值小于1 nM。它能够抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)，引发双链 DNA 断裂和复制突变，从而导致细胞凋亡 (apoptosis)。此外，Prexasertib lactate 还表现出抗肿瘤活性。

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种 ATP 竞争性的、选择性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂 (IC50<1 nM, Ki: 0.9 nM)。Prexasertib Mesylate Hydrate 对 CHK2 (IC50: 8 nM) 和 RSK1 (IC50: 9 nM) 表现出抑制作用。Prexasertib Mesylate Hydrate 能够导致双链 DNA 断裂和复制突变，诱导细胞凋亡，并表现出有效的抗肿瘤作用。