Lometrexol DDATHF|cas:106400-81-1|西域试剂

Lometrexol DDATHF,95.63%

产品编号：Bellancom-14521| CAS NO：106400-81-1| 分子式：C₂₁H₂₅N₅O₆| 分子量：443.45

Lometrexol (DDATHF) 是一种抗嘌呤类抗叶酸药，可通过与甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 紧密结合来抑制 GARFT 的活性。Lometrexol 可以进一步抑制嘌呤从头合成，导致异常的细胞增殖和凋亡，甚至细胞周期停滞。Lometrexol 具有抗癌活性。

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货号	价格	库存与货期
Bellancom-14521	￥2300.00	杭州北京（现货）
Bellancom-14521	￥6900.00	杭州北京（现货）
Bellancom-14521	￥11000.00	杭州北京（现货）

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Lometrexol DDATHF

产品介绍

Lometrexol (DDATHF) 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 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 具有抗癌活性。Lometrexol 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。

生物活性

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

体外研究

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

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

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.

体内研究
(In Vivo)

Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) induces neural tube defects (NTDs) by disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels.
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs).

西域 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)
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)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
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)
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.

体内研究

西域 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)
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)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
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)
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.

体内研究

西域 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)
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)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 40 mg/mL (90.20 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2550 mL	11.2752 mL	22.5505 mL
5 mM	0.4510 mL	2.2550 mL	4.5101 mL
10 mM	0.2255 mL	1.1275 mL	2.2550 mL

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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Xu L, et, al. The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice. Nutr Metab (Lond). 2016 Aug 23;13(1):56. [Content Brief]

. Scaletti E, et, al. Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT2 by antifolate drugs. FEBS Lett. 2019 Jul;593(14):1863-1873. [Content Brief]

. Bronder JL, et, al. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function. Cancer Res. 2002 Sep 15;62(18):5236-41. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Lometrexol
CAS号：	106400-81-1
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Lometrexol
别名：	DDATHF
分子式：	C21H25N5O6
分子量：	443.45

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Xu L, et al. The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice. Nutr Metab (Lond). 2016 Aug 23;13(1):56.

Lometrexol DDATHF,95.63%

Lometrexol DDATHF

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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