中文名称: 洛美曲索水合物
英文名称: Lometrexol hydrate
CAS No: 106400-81-1
分子式: C21H25N5O6.XH2O
分子量: 443.45(anhydrous basis)
L10335 洛美曲索水合物 ≥98% (psaitong)
包装规格:
5mg 25mg in glass bottle
溶解性:
溶于DMSO(≥5mg/mL)
产品描述:

基本信息

产品编号:L10335

产品名称:Lometrexol hydrate

CAS:

106400-81-1

 

储存条件

粉末

2-8℃

四年

 

 

分子式:

C21H25N5O6.XH2O

溶于液体

-80℃

六个月

分子量

443.45

-20℃

一个月

化学名: 

(2S)-2-[[4-[2-[(6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]amino]pentanedioic acid

 

Solubility (25°C)

 

体外

DMSO

40mg/mL (86.68mM; Need ultrasonic and warming

Ethanol

 

Water

 

体内

现配现用

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.1670mL

10.8349mL

21.6699mL

5mM

0.4334mL

2.1670mL

4.3340mL

10mM

0.2167mL

1.0835mL

2.1670mL

 

生物活性

产品描述

一种抗嘌呤类抗叶酸 (antifolate) 药,可抑制甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 的活性,但不会引起可检测水平的 DNA 链断裂。

靶点/IC50

GARFT

 

体外研究

Lometrexol hydrate (DDATHF hydrate) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides .

Lometrexol hydrate (1-30μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells .

Lometrexol hydrate (1μM; 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, 30μM

Incubation Time:

2, 4, 6, 8, 10 hours

Result:

Induced rapid and complete growth inhibition.

Cell Cycle Analysis

Cell Line:

L1210 cells

Concentration:

1μM

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.

 

体内研究

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 60mg/kg

Administration:

Intraperitoneal injection; on gestation day 7.5

Result:

Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.

保存条件:
2-8℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):