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Ceralasertib

产品编号 T3338 CAS 1352226-88-0

别名: AZD6738

Ceralasertib (AZD6738) 是一种具有口服活性的选择性 ATR 激酶抑制剂，IC50 为 1 nM。

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Ceralasertib, CAS 1352226-88-0

规格	价格/CNY	货期
1 mg	￥ 469	现货
2 mg	￥ 671	现货
5 mg	￥ 970	现货
10 mg	￥ 1,516	现货
25 mg	￥ 2,823	现货
50 mg	￥ 3,980	现货
100 mg	￥ 5,680	现货
500 mg	￥ 11,700	现货
1 mL * 10 mM (in DMSO)	￥ 915	现货

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其他形式的 Ceralasertib:

Ceralasertib formate
询价
(S)-Ceralasertib
询价

选择批次

纯度: 99.99%

纯度: 99.91%

纯度: 99.76%

纯度: 99.26%

纯度: 98.46%

纯度: 98%

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	Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM.
靶点活性	ATR:1 nM
体外活性	In four Kras mutant cell lines: H23, H460, A549, and H358,AZD6738 inhibits ATR kinase activity and impairs cell viability. AZD6738 strongly synergizes with cisplatin in an ATM-deficient NSCLC cell line in vitro[1]. In p53 or ATM defective cells, AZD6738 treatment resulted in replication fork stalls and accumulation of unrepaired DNA damage, as evidenced by γH2AX and 53BP1 foci formation, which was carried through into mitosis, resulting in cell death by mitotic catastrophe[2].
体内活性	The combination of 50 mg/kg AZD6738 and cisplatin resulted in a 75.5% mean tumor growth inhibition (TGI) of H460 xenografts at day 14 (P ≤ 0.0001 compared to vehicle). Growth of tumors treated with the combination was also significantly different from that of tumors treated with cisplatin or AZD6738 alone [1]. In LoVo derived mouse xenograft, a combination of AZD6738 (50?mg/kg)?+?IR (2?Gy) can be adjusted to avoid toxicity while still maintaining efficacy[3].
激酶实验	General procedure for the EC50 test: DDR1 is induced by 2 Gg/ml doxycycline for 48 hrs prior to DDR1 activation by rat tail collagen I. The DDR1 over-expressed U2OS is pre-treated by media containing each concentration of the compound for 1 hr and treated by changing the media to the EC50 test media containing 10 Gg/ml collagen and each concentration of the compound for 2 hrs. Each cells is washed with cold PBS three times and lysed with the lysis buffer (50 mMTris, pH 7.5, 1% Triton X-100, 0.1% SDS, 150 mM NaCl, 5 mM EDTA, 100 mMNaF, 2 mM Na3VO4, 1 mM PMSF, 10 Gg/ml aprotinin, and 10 Gg/ml leupeptin). The activation of DDR1 is quantified by density using program ImageJ to determine EC50 following Western blot using anti-activated human DDR1b (Y513).
细胞实验	Cells are treated in white walled, clear bottom 96-well plates with the indicated doses of AZD6738, cisplatin, gemcitabine, or combination for 48 h. ATP levels are assessed as surrogate measure of viability was assessed using the CellTiter-Glo Luminescent Cell Viability Assay and Safire 2 plate reader. Raw data are corrected for background luminescence prior to further analysis. For AZD6738 treatment, log dose response curves are generated in GraphPad Prism 6 by nonlinear regression (log(inhibitor) vs. response with variable slope) of log-transformed (x = log(x)) data normalized to the mean of untreated controls. GI values, defined as the dose X at which Y = 50%, were extrapolated from dose response curves.

别名	AZD6738
分子量	412.51
分子式	C20H24N6O2S
CAS No.	1352226-88-0

存储

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

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 39 mg/mL (94.5 mM)

DMSO: 76 mg/mL (184.2 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.4242 mL	12.1209 mL	24.2418 mL	60.6046 mL
	5 mM	0.4848 mL	2.4242 mL	4.8484 mL	12.1209 mL
	10 mM	0.2424 mL	1.2121 mL	2.4242 mL	6.0605 mL
	20 mM	0.1212 mL	0.606 mL	1.2121 mL	3.0302 mL
	50 mM	0.0485 mL	0.2424 mL	0.4848 mL	1.2121 mL
DMSO	100 mM	0.0242 mL	0.1212 mL	0.2424 mL	0.606 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. Vendetti FP, et al. Oncotarget. 2015. doi: 10.18632/oncotarget.6247. 2. Kwok M, et al. Lancet. 2015. doi: 10.12016/S20140-6736(15)60373-7. 3. Checkley S, et al. Sci Rep. 2015. doi: 10.1038/srep13545. 4. Liang J, Niu Z, Yu X, et al. Counteracting Genome Instability by p53-dependent Mintosis[J]. bioRxiv. 2020. 5. Liang J, Niu Z, Zhang B, et al. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis[J]. Cell Death & Differentiation. 2020: 1-15. 6. Lei H, Xu H Z, Shan H Z, et al. Targeting USP47 overcomes tyrosine kinase inhibitor resistance and eradicates leukemia stem/progenitor cells in chronic myelogenous leukemia[J]. Nature Communications. 2021, 12(1): 1-16

文献引用

1. Lei H, Xu H Z, Shan H Z, et al. Targeting USP47 overcomes tyrosine kinase inhibitor resistance and eradicates leukemia stem/progenitor cells in chronic myelogenous leukemia. Nature Communications. 2021 Jan 4;12(1):51. doi: 10.1038/s41467-020-20259-0. 2. Lei H, Xu H Z, Shan H Z, et al. Targeting USP47 overcomes tyrosine kinase inhibitor resistance and eradicates leukemia stem/progenitor cells in chronic myelogenous leukemia. Nature Communications. 2021 Jan 4;12(1):51. doi: 10.1038/s41467-020-20259-0. 3. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15 4. Liang J, Niu Z, Zhang B, et al Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15.

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

Ceralasertib 1352226-88-0 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR inhibit Ataxia telangiectasia mutated ATM and RAD3 related Inhibitor AZD 6738 AZD-6738 AZD6738 inhibitor

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Ceralasertib

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

文献引用

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