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Prexasertib mesylate (Synonyms: LY2606368 mesylate)
Prexasertib (LY2606368) mesylate 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 mesylate 抑制 chk2 (ic50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib mesylate 引起双链 DNA 断裂和复制突变,导致细胞凋亡 (apoptosis)。Prexasertib mesylate 显示有效的抗肿瘤活性。
Prexasertib mesylate Chemical Structure
CAS No. : 1234015-55-4
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Prexasertib mesylate 的其他形式现货产品:
生物活性 |
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nm. prexasertib mesylate inhibits chk2 (ic50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity[1][2]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Prexasertib (LY2606368) mesylate inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). Prexasertib mesylate requires CDC25A and CDK2 to cause DNA damage[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle Analysis[1]
Western Blot Analysis[1]
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体内研究 (In Vivo) |
Prexasertib mesylate (1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
461.49 |
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Formula |
C19H23N7O5S |
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CAS 号 |
1234015-55-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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