推荐产品
产品名称
洛美曲索水合物, ≥95% (HPLC)
质量水平
方案
≥95% (HPLC)
表单
powder
颜色
white to light yellow
溶解性
DMSO: ≥5 mg/mL
储存温度
2-8°C
SMILES字符串
O.NC1=NC(=O)C2=C(NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C2)N1
InChI
1S/C21H25N5O6.H2O/c22-21-25-17-14(19(30)26-21)9-12(10-23-17)2-1-11-3-5-13(6-4-11)18(29)24-15(20(31)32)7-8-16(27)28;/h3-6,12,15H,1-2,7-10H2,(H,24,29)(H,27,28)(H,31,32)(H4,22,23,25,26,30);1H2/t12-,15+;/m1./s1
InChI key
AEFQSKJUVDZANQ-YLCXCWDSSA-N
应用
使用洛美曲索水合物比较人GARFTase有效抑制剂的生物学活性。
生化/生理作用
甘氨酰胺核糖核苷酸甲酰基转移酶（GARFTase）是从头嘌呤合成所需的叶酸依赖性酶。 洛美曲索是GARFTase的有效抑制剂，但不会干扰叶酸合成中涉及的酶。 已在临床上测试了洛美曲索作为一种类似于甲氨蝶呤的抗叶酸药物，用于治疗各种癌症。 用洛美曲索治疗可迅速降低ATP和GTP水平，使细胞周期停滞并诱导细胞凋亡。 尽管核苷酸库的消耗会诱导p53表达，但洛美曲索在野生型和突变型表达p53的肿瘤细胞中均具有细胞毒性。 洛美曲索对CCRF-CEm白血病细胞具有细胞毒性，IC50为2.9 nM。
甘氨酰胺核糖核苷酸甲酰转移酶抑制剂
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
New agents in cancer clinical trials.
J Adams et al.
Oncogene, 19(56), 6687-6692 (2001-06-28)
Julie L Bronder et al.
Cancer research, 62(18), 5236-5241 (2002-09-18)
The class of folate antimetabolites typified by (6R)-dideazatetrahydrofolate (lometrexol, DDATHF) are specific inhibitors of de novo purine synthesis because of potent inhibition of glycinamide ribonucleotide formyltransferase (GART) but do not induce detectable levels of DNA strand breaks. As such, they
D R Newell
Seminars in oncology, 26(2 Suppl 6), 74-81 (1999-12-22)
Antifolate drugs, as a class, have broad-spectrum activity against both hematologic and solid human malignancies. The pharmacokinetics of the classical antifolate methotrexate have been well-defined and pharmacokinetic data can be exploited to reduce the toxicity and enhance the activity of
X Lu et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 7(7), 2114-2123 (2001-07-13)
The impact of p53 status on cellular sensitivity to antifolate drugs has been examined in seven human cell lines (A549, MCF7, T-47D, CCRF-CEM, COR-L23, A2780, and HCT-116) and p53 nonfunctional counterparts of two of the cell lines (HCT-116/N7 and A2780/CP70).
Huiling Qi et al.
Cancer research, 66(11), 5875-5882 (2006-06-03)
The folate receptor (FR) type beta is a promising target for therapeutic intervention in acute myelogenous leukemia (AML), owing particularly to its selective up-regulation in the leukemic cells by all-trans retinoic acid (ATRA). Here we show, using KG-1 and MV4-11
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