AZD6738
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZD6738是ATR的选择性抑制剂，对于静息CLL细胞的IC50大约为30 μM [1,2]。
ATR是PI3K相关激酶,它参与DNA损伤的修复。在细胞分裂过程中，它补充和激活单链DNA断裂位点以帮助启动DNA修复[1]。
γH2AX是DNA损伤的生物标志物。在再生体外模型中， AZD6738治疗70小时后，γH2AX信号持续发生[1]。复制停滞可能停止DNA双链断裂的形成和共济失调毛细血管扩张症突变（ATM）激酶的活化。作为癌细胞系的单一试剂，AZD6738具有活性。在缺乏ATM通路的细胞系中，AZD6738的敏感性明显增强[3]。
在ATM缺陷而非ATM精通的体内模型中，耐受剂量的AZD6738单独治疗显著抑制肿瘤活性。电离辐射（IR）是DNA损伤诱导剂。当AZD6738和IR共同使用时，观测到消退或抗肿瘤生长抑制活性。在肿瘤组织中，AZD6738与固有的γH2AX染色增加有关。在正常肠组织或骨髓中，AZD6738短暂增加γH2AX染色[3]。
参考文献：
[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.
- 1. Karin Broennimann, Inna Ricardo-Lax, et al. "RNR-R2 Upregulation by a Short Non-Coding Viral Transcript." Biomolecules. 2021 Dec 3;11(12):1822. PMID:34944466
- 2. Inna Ricardo-Lax, Karin Broennimann,et al. "A short HBV RNA region induces RNR-R2 expression in non-cycling cells and in primary human hepatocytes."bioRxiv. 2018 October 31.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 412.51 |
| Cas No. | 1352226-88-0 |
| Formula | C20H24N6O2S |
| Solubility | insoluble in H2O; ≥82 mg/mL in DMSO; ≥82.4 mg/mL in EtOH |
| Chemical Name | (R)-3-methyl-4-(6-(1-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine |
| SDF | Download SDF |
| Canonical SMILES | C[C@H]1N(C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(C5([S@](=O)(C)=N)CC5)=C2)CCOC1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
相关生物数据
相关生物数据
