Prexasertib (LY2606368)是CHK1的ATP竞争性抑制剂，Ki值为0.9 nM。在cell-free实验中，LY2606368对CHK2和RSK的IC50值分别为8 nM和9 nM。 Information Prexasertib (LY2606368) is an ATP-competitiveCHK1inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. Targets Chk1 (Cell-free assay); Chk2 (Cell-free assay); RSK (Cell-free assay) 0.9 nM(Ki); 8 nM; 9 nM In vitro In nonclinical studies, LY2606368 induced DNA damage as measured by replication catastrophe and increases in pH2A.X, a marker of double-stranded DNA breaks. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, LY2606368 potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. LY2606368 was broadly antiproliferative with IC50 values typically 1,000 nmol/L. LY2606368 requires CDC25A and CDK2 to cause DNA damage. In vivo LY2606368 inhibited tumor growth in cancer xenografts as monotherapy and in combination with other agents. In an orthotopic SKOV3 ovarian cancer model, LY2606368 was shown to inhibit the growth of primary tumors and significantly reduce the incidence of metastases and ascites accumulation. LY2606368 also demonstrated efficacy in an SW1990 orthotopic pancreatic cancer model resulting in a 92% inhibition of primary tumor growth and the elimination of metastases to the lymphnode, spleen, and intestine. Cell Research(from reference) Cell lines：HeLa cells Concentrations：33 or 100 nmol/L Incubation Time：12 h
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Prexasertib dihydrochloride
Dangerous GoodsCAS number：1234015-54-3 molecular formula：C18H19N7O2.2HCl
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| Chinese alias | 普雷沙替布二盐酸盐 | ||
| English alias | LY2606368 diHCl | LY2606368 Prexasertib HCl | 9RFT476U2L | LY2606368 2HCl | EX-A758A | 2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-, hydrochloride (1:2) | LY2606368 dihydrochloride | LY-2606368 dihydrochloride | ||
| CAS number | 1234015-54-3 | molecular formula | C18H19N7O2.2HCl |
| molecular weight | 438.31 g/mol | Exact mass | ≥98% |
| PSA | 135.000 Ų | logp | - |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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