Nolatrexed (AG-337)
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.
IC50:对L1210\CCRF-CEM和GC3/M TK细胞系的IC50分别为1.0\0.81和1.0 μM.
胸苷酸合成酶(TS)是合成2'-脱氧胸苷-5'-单磷酸的关键酶,2'-脱氧胸苷-5'-单磷酸是用于DNA生物合成的必需前体.因此,该酶是癌症化疗的关键靶标.Nolatrexed (AG-337)是一种非经典胸苷酸合成酶抑制剂.
体外实验:Nolatrexed是依据TS分子模型和叶酸结合位点的X射线晶体学数据设计的.它是一种非经典的TS抑制剂,缺乏末端谷氨酸侧链,在生理pH下不带电荷.Nolatrexed进入细胞不需要特定的运输机制,进入细胞后,不是叶酰聚谷氨酸合成酶的底物[1].
在体实验:使用nolatrexed治疗Bu25TK肿瘤异种移植裸鼠,观察到其抗肿瘤活性时间依赖性增加[1].
临床试验:I期临床研究表明,给予肿瘤患者连续静脉内输注800 mg/m2/d 的Nolatrexed超过5天具有安全性,给药时间与抗肿瘤效应相关[2].
参考文献：
[1] Hughes AN, Rafi I, Griffin MJ, Calvert AH, Newell DR, Calvete JA, Johnston A, Clendeninn N, Boddy AV. Phase I studies with the nonclassical antifolate nolatrexed dihydrochloride (AG337, THYMITAQ) administered orally for 5 days. Clin Cancer Res. 1999 Jan;5(1):111-8.
[2] Rafi I, Boddy AV, Calvete JA, Taylor GA, Newell DR, Bailey NP, Lind MJ, Green M, Hines J, Johnstone A, Clendeninn N, Calvert AH. Preclinical and phase I clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors. J Clin Oncol. 1998 Mar;16(3):1131-41.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 357.26 |
| Cas No. | 152946-68-4 |
| Formula | C14H14Cl2N4OS |
| Solubility | ≥108.6 mg/mL in H2O; ≥17.2 mg/mL in DMSO; ≥5.5 mg/mL in EtOH with ultrasonic |
| Chemical Name | 2-imino-6-methyl-5-(pyridin-4-ylthio)-1,2-dihydroquinazolin-4-ol dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(SC2=CC=NC=C2)C(C(O)=NC3=N)=C(N3)C=C1.Cl.Cl |
| 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
- 批次:
化学结构
