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106400-81-1

中文名稱 洛美曲索
CAS 106400-81-1
分子式 C21H25N5O6
分子量 443.45
MOL 文件 106400-81-1.mol
更新日期 2023/03/20 15:41:25
106400-81-1 結(jié)構(gòu)式 106400-81-1 結(jié)構(gòu)式

基本信息

中文別名
洛美曲索
洛美曲索水合物
英文別名
LY 264618
Lometrexol
Lometrexolum
LY 264618 hydrate
Lometrexol hydrate
Lometrexol(LY 264618)
Lometrexolum [inn-latin]
(6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid
N-[4-[2-[[(R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid
L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-

物理化學性質(zhì)

密度1.56±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度二甲基亞砜:≥5mg/mL
酸度系數(shù)(pKa)3.60±0.10(Predicted)
形態(tài)粉末
顏色白色至淺黃色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
防范說明P301+P310
危險品標志T
危險類別碼25
安全說明45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3
洛美曲索價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-14521洛美曲索
Lometrexol
106400-81-11mg860元
2024/11/08HY-14521洛美曲索
Lometrexol
106400-81-15mg1950元
2024/11/08HY-14521洛美曲索
Lometrexol
106400-81-110mM * 1mLin DMSO2145元

常見問題列表

生物活性
Lometrexol hydrate (DDATHF hydrate) 是一種抗嘌呤類抗葉酸 (antifolate) 藥,可抑制甘氨酰胺核糖核苷酸甲酰基轉(zhuǎn)移酶 (GARFT) 的活性,但不會引起可檢測水平的 DNA 鏈斷裂。Lometrexol hydrate 可以進一步抑制嘌呤從頭合成,導致異常的細胞增殖,凋亡 (apoptosis) 和細胞周期停滯。Lometrexol hydrate 具有抗癌活性。Lometrexol hydrate 還是一種有效的人絲氨酸羥甲基轉(zhuǎn)移酶 1/2 (hSHMT1/2) 抑制劑。
靶點

GARFT

體外研究

Lometrexol hydrate (DDATHF hydrate) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides.
Lometrexol hydrate (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells.
Lometrexol hydrate (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells.
Lometrexol hydrate induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs).

Cell Viability Assay

Cell Line: Mouse leukemia L1210 cells
Concentration: 1, 30 μM
Incubation Time: 2, 4, 6, 8, 10 hours
Result: Induced rapid and complete growth inhibition.

Cell Cycle Analysis

Cell Line: L1210 cells
Concentration: 1 μM
Incubation Time: 2, 4, 8, 12, 24 hours
Result: Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase.
體內(nèi)研究

Lometrexol hydrate (DDATHF hydrate; i.p.; 15-60 mg/kg; on gestation day 7.5) increases the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Lometrexol hydrate (i.p.; 40 mg/kg) maximally inhibits GARFT activity after at 6 hours and thereafter gradually increases with time but remains significantly lower than control even at 96 hours. Levels of ATP, GTP, dATP and dGTP of NTDs embryonic brain tissue decreases significantly at 6 h, and more significantly over time.

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)
Dosage: 15, 30, 35, 40, 45 and 60 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
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