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AZD6738 Sale

(Synonyms: AZD6738) 目录号 : GC16941

An ATR kinase inhibitor

AZD6738 Chemical Structure

Cas No.:1352226-88-0

规格 价格 库存 购买数量
5mg
¥1,061.00
现货
25mg
¥3,224.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Ceralasertib (AZD6738) is dissolved in DMSO at 30 mM and diluted in DMSO to desired working concentrations. The final DMSO concentration in media for all conditions and controls is 0.1% for Ceralasertib (AZD6738) dose response experiments, 0.05% for Ceralasertib (AZD6738) + chemotherapy viability experiments, and 0.025% for all experiments involving 0.3 μM and 1.0 μM doses of Ceralasertib (AZD6738)[1].

Animal experiment:

Mice[1]Ceralasertib (AZD6738) is dissolved in DMSO at a concentration of 25 mg/mL or 50 mg/mL and diluted 1:5 in propylene glycol. Ceralasertib (AZD6738) is administered by oral gavage at 25 mg/kg (H23) or 50 mg/kg (H460) for 14 consecutive days. The dosing volume is 10 mL/kg.[1].

References:

[1]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo.
[2]. Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119.

产品描述

AZD6738 is a selective ATR (Ataxia Telangiectasia and RAD3-related) inhibitor, with an IC50 of approximately 30 uM to resting CLL cells [1] [2].

ATR is a PI3K-related kinase. It is involved in the repair of DNA damage. During cell division, it is recruited and activated at sites of single strand DNA breaks to help initiate DNA repair [1].

γH2AX acts as a biomarker of DNA damage. In an in vitro model capable of reproducing, over 70 hours after the initiation of the treatment with AZD6738, the γH2AX signal was sustained [1]. Stalled replication forks may collapse the formation of DNA double stranded breaks and the activation of the ataxia telangiectasia mutated (ATM) kinase. As a single agent across cancer cell line panels, AZD6738 is active. In cell lines lacking ATM-pathway, the sensitivity of AZD6738 was enhanced [3].

In ATM-deficient but not ATM-proficient in vivo models, treatment with AZD6738 alone significantly inhibited the activity of tumors in equivalent, tolerated doses. Ionizing radiation (IR) is a DNA damaging inducing agent. When AZD6738 and IR were used together, regression or anti-tumor growth inhibitory activity was observed. In tumor tissue, AZD6738 is associated with a persistent γH2AX staining increase. In normal gut tissue or bone marrow, treatment with AZD6738 only transiently increased the γH2AX staining [3].

References:
[1].  Choi MY, Fecteau JF, Brown J, et al. Induction of proliferation sensitizes chronic lymphocytic leukemia cells to apoptosis mediated by the ATR inhibitor AZD6738. Cancer Research, 2014, 74(19 Supplement): 5485-5485.
[2].  Checkley S, MacCallum L, Yates J, et al. Bridging the gap between in vitro and in vivo: Dose and schedule predictions for the ATR inhibitor AZD6738. Scientific reports, 2015, 5.
[3].  Guichard SM, Brown E, Odedra R, et al. The pre-clinical in vitro and in vivo activity of AZD6738: A potent and selective inhibitor of ATR kinase. Cancer Research, 2013, 73(8 Supplement): 3343-3343.

Chemical Properties

Cas No. 1352226-88-0 SDF
别名 AZD6738
化学名 (R)-3-methyl-4-(6-(1-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine
Canonical SMILES C[C@H]1N(C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(C5([S@](=O)(C)=N)CC5)=C2)CCOC1
分子式 C20H24N6O2S 分子量 412.51
溶解度 ≥ 82 mg/mL in DMSO, ≥ 82.4 mg/mL in EtOH 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4242 mL 12.1209 mL 24.2418 mL
5 mM 0.4848 mL 2.4242 mL 4.8484 mL
10 mM 0.2424 mL 1.2121 mL 2.4242 mL
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