Lomeguatrib
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.
Lomeguatrib是O6-烷基胺-DNA-甲基转移酶(MGMT)的抑制剂[1],在MCF-7细胞中有效灭活MGMT的IC50值约为6 nM[2]。
MGMT活性与MTIC(达卡巴嗪的代谢产物)介导的DNA损伤密切相关[1]。
Lomeguatrib可使含有MGMT活性的A375P细胞对替莫唑胺(TMZ)敏感,但对达卡巴嗪(DTIC)的效果没有影响。在其它mutBRAF细胞和几种mutNRAS细胞系如WM1361中也得到了类似的结果[1]。
患者用lomeguatrib治疗后PBMC中MGMT无活性或活性很低。Lomeguatrib使用量为20 mg时,携带CNS肿瘤的患者只有16.7 fmol/μg的DNA活性MGMT。该患者有25%的无活性肿瘤MGMT。这一比例比同等lomeguatrib剂量下的另外两个CNS病人要低。不同的肿瘤类型具有显著不同的总肿瘤MGMT。前列腺癌最高(554 ± 404 fmol/mg蛋白),CNS肿瘤最低(89.9 ± 44.5 fmol/mg蛋白),结肠癌肿瘤的总蛋白水平则居中(244 ± 181 fmol/mg蛋白)。在结肠癌、初发的CNS肿瘤和前列腺癌病人中,无活性MGMT的比例随lomeguatrib剂量的增加而增加[3]。
参考文献:
[1]. Imanol Arozarena, Ibai Goicoechea, Oihane Erice, et al. Differential chemosensitivity to antifolate drugs between RAS and BRAF melanoma cells. Molecular Cancer, 2014, 13:154.
[2]. M Clemons, J Kelly, AJ Watson, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. British Journal of Cancer, 2005, 93:1152-1156.
[3]. Amanda J. Watson, Ami Sabharwal, Mary Thorncroft, et al. Tumor O6-methylguanine-DNA Methyltransferase Inactivation by Oral Lomeguatrib. Clinical Cancer Research, 2010, 16(2):743-9.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 326.17 |
Cas No. | 192441-08-0 |
Formula | C10H8BrN5OS |
Solubility | ≥50 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | 6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine |
SDF | Download SDF |
Canonical SMILES | C1=C(SC=C1Br)COC2=NC(=NC3=C2NC=N3)N |
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。 |
Description | Lomeguatrib是一种有效的O6-烷基胺-DNA-烷基转移酶抑制剂,IC50值为5 nM。 | |||||
靶点 | O6-alkylguanine-DNA-alkyltransferase | |||||
IC50 | 5 nM |
质量控制和MSDS
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