SML0040
洛美曲索水合物
≥95% (HPLC), powder, GARFTase inhibitor
别名:
LY 264618水合物, N-[4-[2-[(6R)-2-氨基-3,4,5,6,7,8-四氢-4-氧吡啶并[2,3-d]嘧啶-6-基]乙基]苯甲酰基]-L-谷氨酸水合物
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关于此项目
经验公式（希尔记法）:
C21H25N5O6 · xH2O
化学文摘社编号:
分子量:
443.45 (anhydrous basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
产品名称
洛美曲索水合物, ≥95% (HPLC)
SMILES string
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
assay
≥95% (HPLC)
form
powder
color
white to light yellow
solubility
DMSO: ≥5 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
Application
使用洛美曲索水合物比较人GARFTase有效抑制剂的生物学活性。
Biochem/physiol Actions
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
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
R Zhao et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 6(8), 3304-3311 (2000-08-24)
A murine leukemia cell line was identified that is highly resistant to methotrexate (MTX), due to impaired transport, but fully sensitive to 5,10-dideazatetrahydrofolate (DDATHF). A valine-to-methionine substitution at amino acid 104 in the reduced folate carrier (RFC1) explains this disparity
A Tse et al.
The Journal of biological chemistry, 273(40), 25944-25952 (1998-09-25)
Mouse L1210 cell variants were selected for resistance to 5, 10-dideazatetrahydrofolate, a potent inhibitor of the first folate-dependent enzyme in de novo purine synthesis, glycinamide ribonucleotide formyltransferase. The drug-resistant phenotype selected was conditional to the folate compound used to support
A Strømhaug et al.
Cancer chemotherapy and pharmacology, 45(6), 450-456 (2000-06-15)
Since the clinical introduction of the antifolates aminopterin (AMT) and methotrexate (MTX) many promising analogs have been developed. A common feature of these compounds is their ability to induce bone marrow suppression. However, few studies have been undertaken on the
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
T W Synold et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 4(10), 2349-2355 (1998-10-31)
Lometrexol inhibits the first folate-dependent enzyme in de novo purine biosynthesis and is avidly polyglutamated and retained in tissues expressing folylpolyglutamate synthetase. Although clinical studies have been limited by cumulative toxicity, preclinical studies show that pretreatment with folic acid can
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