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Prexasertib dihydrochloride

产品编号 T4327 CAS 1234015-54-3

别名: LY2606368 (dihydrochloride), Prexasertib HCl, LY2606368

Prexasertib dihydrochloride (LY2606368) 是一种选择性的，ATP 竞争性的细胞周期检测点激酶 1 抑制剂，Ki 为 0.9 nM，IC50为 <1 nM。它抑制 CHK2(IC50=8 nM) 和 RSK1 (IC50=9 nM)。它引起双链 DNA 断裂和复制突变，导致细胞凋亡，有抗肿瘤活性。

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Prexasertib dihydrochloride Chemical Structure

Prexasertib dihydrochloride, CAS 1234015-54-3

规格	价格/CNY	货期
1 mg	￥ 398	现货
2 mg	￥ 578	现货
5 mg	￥ 1,080	现货
10 mg	￥ 1,770	现货
25 mg	￥ 3,820	现货
50 mg	￥ 5,550	现货
100 mg	￥ 7,770	现货
500 mg	￥ 15,500	现货
1 mL * 10 mM (in DMSO)	￥ 1,260	现货

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其他形式的 Prexasertib dihydrochloride:

Prexasertib
现货
Prexasertib lactate hydrate
询价
Prexasertib Mesylate Hydrate
询价
LY2606368 HCl (1234015-52-1 free base)
询价
Prexasertib dimesylate
询价
Prexasertib mesylate
询价

选择批次

纯度: 99.82%

纯度: 99.17%

纯度: 97.5%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.
靶点活性	Chk1:0.9 nM, RSK:9 nM, Chk2:8 nM
体外活性	LY2606368 induces DNA damage and increases in pH2A.X. In cells, LY2606368 causes the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, LY2606368 effectively abrogates the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells (EC50: 9 nM). LY2606368 was broadly antiproliferative in the most sensitive cell lines (IC50s<50 nM) with a minority of cell lines showing considerable resistance (IC50s >1,000 nM). LY2606368 requires CDK2 and CDC25A to cause DNA damage.
体内活性	In cancer xenografts, LY2606368 inhibits tumor growth by monotherapy and combined with other agents. In an orthotopic SKOV3 ovarian cancer model, LY2606368 inhibits the growth of primary tumors and markedly reduces the incidence of metastases and ascites accumulation. In an SW1990 orthotopic pancreatic cancer model, LY2606368 also causes a 92% inhibition of primary tumor growth and the elimination of metastases to the lymph node, spleen, and intestine.
激酶实验	The interaction of COTI-2 with 227 kinases is tested using the AMBIT BIOSCIENCES KINOMESCAN assay. In brief, streptavidin-coated magnetic beads are treated with biotinylated small molecule ligands for 30 min at 25°C to generate affinity resins for kinase assays. The liganded beads are blocked with excess biotin and washed with blocking buffer (1% BSA, 0.05% Tween 20, 1 mM DTT) to remove unbound ligand and to reduce non-specific binding. Binding reactions are assembled by combining phage lysates, liganded affinity beads, and COTI-2 in 1× binding buffer (20% SeaBlock, 0.17× PBS, 0.05% Tween 20, 6 mM DTT). All reactions are carried out in polystyrene 96-well plates that have been pre-treated with blocking buffer in a final volume of 0.1 mL.
细胞实验	HeLa cells were plated onto T25 flasks and allowed to recover for 24 hours.LY2606368 was then added to give final concentrations of 33 or 100 nmol/L.In some experiments,20 μMol/L Z-VAD-FMK was included during the drug treatment.Cells were treated for 12 hours,and during the last 2 hours,colchicine was added to 1 μg/mL.Fixation of nuclei for metaphase spreads was done following the method of Bayani and Squire.Chromosome spreads were done.A 12-μL volume of cell suspension in 3:1 methanol/acetic acid fixative was dropped from a height of 3 cm onto dry glass slides or coverslips.The slides were then heated for 45 seconds on a 43°C metal block,before being removed to allow drying to complete at room temperature.Coverslips were mounted on slides with Vectashield Hard Set mounting medium with DAPI.Slides were examined with a Leica DMR fluorescence microscope and images were captured using a SPOT RT3 Slider camera.
动物实验	LY2606368 is formulated in a vehicle consisting of 20% Captisol.Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight and placed into their respective treatment groups. The vehicle consisting of 20% Captisol pH4 or LY2606368 is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates were analyzed by immunoblot analysis for protein phosphorylation levels.

别名	LY2606368 (dihydrochloride), Prexasertib HCl, LY2606368
分子量	438.31
分子式	C18H21Cl2N7O2
CAS No.	1234015-54-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL(68.4 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2815 mL	11.4075 mL	22.8149 mL	57.0373 mL
	5 mM	0.4563 mL	2.2815 mL	4.563 mL	11.4075 mL
	10 mM	0.2281 mL	1.1407 mL	2.2815 mL	5.7037 mL
	20 mM	0.1141 mL	0.5704 mL	1.1407 mL	2.8519 mL
	50 mM	0.0456 mL	0.2281 mL	0.4563 mL	1.1407 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Hong D,etal.Phase I Study of LY2606368, a Checkpoint Kinase 1 Inhibitor, in Patients With Advanced Cancer.J Clin Oncol. 2016 May 20;34(15):1764-71. 2. King C,etal.LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms.Mol Cancer Ther. 2015 Sep;14(9):22004-13. 3. McNeely S,etal.CHEK again: revisiting the development of CHK1 inhibitors for cancer therapy.Pharmacol Ther. 2014 Apr;142(1):1-10. 4. Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Prexasertib dihydrochloride 1234015-54-3 Apoptosis Cell Cycle/Checkpoint MAPK PI3K/Akt/mTOR signaling Chk S6 Kinase CDK2 ARK5 replication RSK1 inhibit MELK DNA LY2606368 (dihydrochloride) HeLa Inhibitor Prexasertib HCl HT-29 Prexasertib Dihydrochloride double-stranded BRSK2 ATP-competitive CDC25A S296 S516 autophosphorylation H2AX LY 2606368 LY-2606368 LY2606368 SIK Checkpoint Kinase (Chk) Prexasertib inhibitor

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Prexasertib dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords