L2518557计算溶液所需的质量、体积或浓度。
Prexasertib dimesylate
有货
概述
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis . Prexasertib dimesylate shows potent anti-tumor activity
In Vitro
Prexasertib dimesylate (LY2606368 dimesylate) inhibits MELK (IC 50 =38 nM), SIK (IC 50 =42 nM), BRSK2 (IC 50 =48 nM), ARK5 (IC 50 =64 nM). Prexasertib dimesylate requires CDC25A and CDK2 to cause DNA damage. Prexasertib dimesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells. Prexasertib dimesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells. Prexasertib dimesylate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells. Prexasertib dimesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib dimesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: HeLa cells Concentration: 33, 100 nM Incubation Time: For 7 hours Result: Had an IC 50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis. Western Blot AnalysisCell Line: HT-29 cells Concentration: 8, 16, 31, 63, 125, 250 nM Incubation Time: Pre-treated for 15 minutes Result: Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC 50 of less than 31 nM) in HT-29 cells.
In Vivo
Prexasertib dimesylate (LY2606368 dimesylate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts . Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells Dosage: 1, 3.3, or 10 mg/kg Administration: SC; twice daily for 3 days, rest 4 days; for three cycles Result: Caused statistically significant tumor growth inhibition (up to 72.3%). Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells Dosage: 15 mg/kg (Pharmacokinetic Analysis) Administration: SC (200 μL) Result: CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures. Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
Form:Solid
IC50& Target:Chk1 0.9 nM (Ki) Chk1 <1 nM (IC 50 ) Chk2 8 nM (IC 50 )
规格
别名
普雷沙替布二甲磺酸盐
英文别名
5-((5-(2-(3-Aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile dimethanesulfonate
规格或纯度
Moligand™, ≥99%
英文名称
Prexasertib dimesylate
生化机理
Prexasertib dimesylate（LY2606368 dimesylate）是一种选择性的 ATP 竞争性第二代检查点激酶 1（CHK1）抑制剂，其 K i 为 0.9 nM，IC 50 小于 1 nM。Prexasertib dimesylate 可抑制 CHK2（IC 50 =8 nM）和 RSK1（IC 50 =9 nM）。前
储存条件
2-8°C储存,充氩
运输条件
低温运输
纯度
≥99%
名称和识别符
PubChem SID
分子类型
小分子
IUPAC Name
5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile;methanesulfonic acid
INCHI
1S/C18H19N7O2.2CH4O3S/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17;2*1-5(2,3)4/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25);2*1H3,(H,2,3,4)
InChi Key
HXYBEKZGRNUTBN-UHFFFAOYSA-N
Smiles
COC1=C(C(=CC=C1)OCCCN)C2=CC(=NN2)NC3=NC=C(N=C3)C#N.CS(=O)(=O)O.CS(=O)(=O)O
PubChem CID
分子量
557.60
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
DMSO : 100 mg/mL (179.34 mM; Need ultrasonic) H2O : 50 mg/mL (89.67 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）