Prexasertib dimesylate,Prexasertib dimesylate

Prexasertib dimesylate|T38620|TargetMol

價格	￥1620	￥913	￥554
包裝	10mg	5mg	2mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:Prexasertib dimesylate	英文名稱:Prexasertib dimesylate
CAS:1234015-58-7	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號: T38620

Product Introduction

Bioactivity

名稱	Prexasertib dimesylate
描述	Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective ATP-competitive second-generation inhibitor of checkpoint kinase 1 (CHK1). With a K i of 0.9 nM and an IC 50 of <1 nM, Prexasertib dimesylate effectively inhibits CHK2 (IC 50 = 8 nM) and RSK1 (IC 50 = 9 nM). Its mechanism of action involves inducing double-stranded DNA breakage and replication catastrophe, ultimately leading to apoptosis. Moreover, Prexasertib dimesylate demonstrates potent anti-tumor activity.
體外活性	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[1]. Prexasertib dimesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1]. Prexasertib dimesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1]. 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[1]. 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[1]. Cell Cycle Analysis[1]Cell 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 Analysis[1]Cell 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.
體內活性	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[1]. Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1]. Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]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[1]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.
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關鍵字	LY2606368 Dimesylate \| Prexasertib \| Prexasertib dimesylate \| LY2606368 \| LY-2606368 Dimesylate \| LY-2606368 \| LY 2606368 \| Prexasertib Dimesylate \| LY 2606368 Dimesylate

關鍵字： LY2606368 dimesylate|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領域科學家的研究提供專業(yè)的產(chǎn)品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學試劑盒等，此外，我們還建設有CADD（計算機輔助藥物設計）研究中心、藥理實驗室、藥化合成平臺三大技術中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質的產(chǎn)品和服務、快速高效的全球供應鏈和專業(yè)的技術支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結果。

成立日期	2013-04-18 （12年）	注冊資本	589.8595萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	中間體,天然產(chǎn)物,生物化工,化學試劑,生物技術服務	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務

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公司成立：12年
注冊資本：589.8595萬人民幣
企業(yè)類型：有限責任公司(自然人投資或控股)
主營產(chǎn)品：抑制劑&激動劑，天然產(chǎn)物，重組蛋白，化合物庫，技術服務
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Prexasertib dimesylate|T38620|TargetMol相關廠家報價

產(chǎn)品名稱	價格		公司名稱	報價日期
GZD824 Dimesylate (Bcr-Abl抑制劑)	詢價		碧云天生物技術有限公司	2024-12-25

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