2. Cell Cycle/DNA Damage Apoptosis
  3. Antifolate Apoptosis Caspase Bcl-2 Family
  4. Lometrexol hydrate

Lometrexol hydrate  (Synonyms: DDATHF hydrate)

目录号: HY-14521B 纯度: ≥99.0%
COA 产品使用指南

摩尔计算器

Lometrexol (DDATHF) hydrate 是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。Lometrexol hydrate 可以进一步抑制嘌呤从头合成，导致异常的细胞增殖，凋亡 (apoptosis) 和细胞周期停滞。Lometrexol hydrate 具有抗癌活性。Lometrexol hydrate 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。

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Lometrexol hydrate Chemical Structure

Lometrexol hydrate Chemical Structure

CAS No. : 1435784-14-7

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规格 价格 是否有货 数量
1 mg ￥2300
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5 mg ￥6900
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Other Forms of Lometrexol hydrate:

Lometrexol hydrate 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3].

体外研究
(In Vitro)

Lometrexol (DDATHF) hydrate 与 GART 紧密结合，导致细胞内嘌呤核糖核苷酸快速和长时间消耗[3]。
Lometrexol (1-30 μM；2-10 小时) hydrate 诱导L1210 细胞的快速和完全生长抑制[3]。
Lometrexol (1 μM；2-24 小时) hydrate 诱导小鼠白血病 L1210 细胞的细胞周期停滞[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lometrexol hydrate 相关抗体:

Cell Viability Assay[3]

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[3]

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.
体内研究
(In Vivo)

Lometrexol (DDATHF；腹腔注射；15-60 mg/kg；在妊娠第 7.5 天) hydrate 通过干扰嘌呤代谢诱导神经管缺陷 (NTD)，并以剂量依赖的方式增加胚胎吸收率和生长迟缓[1]。
Lometrexol (ip；40 mg/kg；在妊娠第 7.5 天) hydrate 降低甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 活性和 ATP、GTP、dATP 和 dGTP 水平的变化[1]。
Lometrexol (腹腔注射；40 mg/kg；妊娠7.5天) hydrate 诱导神经管缺陷 (NTDs) 异常增殖和凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
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.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.
Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 4 days
Result: Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
Clinical Trial
分子量

461.47

Formula

C21H27N5O7
CAS 号
性状

固体

颜色

White to off-white

中文名称

洛美曲索水合物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 40 mg/mL (86.68 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1670 mL 10.8349 mL 21.6699 mL
5 mM 0.4334 mL 2.1670 mL 4.3340 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.20%

COA (261 KB)

产品使用指南 (1538 KB)
参考文献

Lometrexol hydrate 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1670 mL 10.8349 mL 21.6699 mL 54.1747 mL
5 mM 0.4334 mL 2.1670 mL 4.3340 mL 10.8349 mL
10 mM 0.2167 mL 1.0835 mL 2.1670 mL 5.4175 mL
15 mM 0.1445 mL 0.7223 mL 1.4447 mL 3.6116 mL
20 mM 0.1083 mL 0.5417 mL 1.0835 mL 2.7087 mL
25 mM 0.0867 mL 0.4334 mL 0.8668 mL 2.1670 mL
30 mM 0.0722 mL 0.3612 mL 0.7223 mL 1.8058 mL
40 mM 0.0542 mL 0.2709 mL 0.5417 mL 1.3544 mL
50 mM 0.0433 mL 0.2167 mL 0.4334 mL 1.0835 mL
60 mM 0.0361 mL 0.1806 mL 0.3612 mL 0.9029 mL
80 mM 0.0271 mL 0.1354 mL 0.2709 mL 0.6772 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lometrexol1435784-14-7DDATHF洛美曲索水合物AntifolateApoptosisCaspaseBcl-2 FamilyantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestleukemiaL1210Inhibitorinhibitorinhibit

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目录号：
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