Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种有效、选择性、 ATP 竞争性的 CHK1 和 CHK2 抑制剂，对 CHK1 的 Ki 值为 0.9 nM，IC50 值<1 nm，对 chk2 的 ic50 值为 8 nm。prexasertib mesylate hydrate 抑制 ht-29 细胞 chk1 (s296) 和 (s516) 的自身磷酸化。prexasertib 具有高效抗肿瘤活性，在 hela 细胞中，消除 g2 m 检查点，ec50 9nm。
CAS：1234015-57-6
分子式：C19H25N7O6S
分子量：479.51
纯度：98%
存储：Store at -20°C

Background:

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of<1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1]. Chk1|0.9 nM (Ki)|Chk1|<1 nM (IC50)|Chk2|8 nM (IC50)

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is an ATP competitive CHK1 inhibitor, with a Ki of 0.9 nM and an IC50 of<1 nM[1].Prexasertib (LY2606368) shows high anti-tumor activity against U-2 OS, Calu-6 and HeLa cells (IC50, 3, 3, 37 nM, respectively), causes DNA damage during S-phase requiring CDC25A and CDK2 at 4 μM[1].Prexasertib (0-20 nM) synergizes with olaparib (0-20 μM) to decrease cell viability in HGSOC cells[2].

[1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13. [2]. Brill E, et al. Prexasertib, a cell cycle checkpoint kinases 1 and 2 inhibitor, increases in vitro toxicity of PARP inhibition by preventing Rad51 foci formation in BRCA wild type high-grade serous ovarian cancer. Oncotarget. 2017 Oct 31;8(67):111026-111040.