Prexasertib
Cat. No.：YN270360
| 产品名称: | Prexasertib |
| CAS No.: | 1234015-52-1 |
| Chemical Name: | 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile |
| Synonyms: | LY2606368 |
| 分子量: | 365.39 |
| 分子式: | C₁₈H₁₉N₇O₂ |
| SMILES: | NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Prexasertib (LY2606368) 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 抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib 引起双链 DNA 断裂和复制突变，导致细胞凋亡 (apoptosis)。Prexasertib 显示有效的抗肿瘤活性。 |
| IC50和靶点: | [{name:"Chk1:0.9 nM (Ki)"},{name: "Chk1:<1 nM (IC50)"},{name: "Chk2:8 nM (IC50)"}] |
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King, C., Diaz, H.B., McNeely, S., et al.LY2606368 causes replication catastrophe and antitumor effects through CHK1-dependent mechanismsMol. Cancer Ther.14(9),2004-2013(2015)
Manic, G., Signore, M., Sistigu, A., et al.CHK1-targeted therapy to deplete DNA replication-stressed, p53-deficient, hyperdiploid colorectal cancer stem cellsGut67(5),903-917(2017)
Yin, Y., Shen, Q., Zhang, P., et al.Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancerAm. J. Cancer Res.7(3),473-483(2017)
