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
Robert Mauritz et al.
Biochemical pharmacology, 63(2), 105-115 (2002-02-14)
We determined the mechanisms of resistance of human CCRF-CEM leukemia cells to methotrexate (MTX) vs. those to six novel antifolates: the polyglutamatable thymidylate synthase (TS) inhibitors ZD1694, multitargeted antifolate, pemetrexed, ALIMTA (MTA) and GW1843U89, the non-polyglutamatable inhibitors of TS, ZD9331
New agents in cancer clinical trials.
J Adams et al.
Oncogene, 19(56), 6687-6692 (2001-06-28)
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
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).
L G Mendelsohn et al.
Seminars in oncology, 26(2 Suppl 6), 42-47 (1999-12-22)
The pyrrolopyrimidine-based antifolate, N-¿4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl ]benzoyl¿glutamic acid, LY231514 (MTA) has demonstrated antitumor activity in a broad array of human tumors, including breast cancer, colon cancer, non-small cell lung cancer, head and neck cancer, pancreatic cancer, and other solid tumors. The biochemical
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