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亚叶酸钙水合物 /Folinic acid calcium salt pentahydrate {[allProObj[0].p_purity_real_show]}

货号:A246079 同义名: 亚叶酸钙五水合物 / Leucovorin Calcium Pentahydrate;Leucovorin calcium salt pentahydrate

Folinic acid is a reduced folic acid, which is used in combination with other chemotherapy drugs.

Folinic acid calcium salt pentahydrate 化学结构 CAS号:6035-45-6
Folinic acid calcium salt pentahydrate 化学结构
CAS号:6035-45-6
Folinic acid calcium salt pentahydrate 3D分子结构
CAS号:6035-45-6
Folinic acid calcium salt pentahydrate 化学结构 CAS号:6035-45-6
Folinic acid calcium salt pentahydrate 3D分子结构 CAS号:6035-45-6
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Folinic acid calcium salt pentahydrate 纯度/质量文件 产品仅供科研

货号:A246079 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DHFR 其他靶点 纯度
Pralatrexate 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

99.9%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

99+%
Methotrexate +

hDHFR, IC50: 24 nM

99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Folinic acid calcium salt pentahydrate 生物活性

描述 The biologically active form of folic acid is tetrahydrofolate which is essential for DNA synthesis. Tetrahydrofolate is oxidised to dihydrofolate during DNA synthesis and is regenerated to its active form by the enzyme dihydrofolate reductase. Inhibition of this enzyme prevents DNA synthesis and causes failure of cell renewal. This leads to breaks in epithelial surfaces resulting in oropharyngeal and intestinal ulceration. Methotrexate (MTX) is the most powerful antagonist to inhibit dihydrofolate reductase. Folinic acid is an analogue of tetrahydrofolate and so bypasses the dihydrofolate reductase block. It thus supplies the tetrahydrofolate compounds needed for DNA synthesis [3]. Treatment with folinic acid calcium pentahydrate (CF) could cause improved development in the heart and vessels in MTX-treated embryos, which proved that MTX induced the malformations by inhibiting dihydrofolate reductase (DHFR). The transcript levels of genes such as hand2, mef2a, mef2c, and flk-1 were reduced in MTX-treated embryos. Compared with the MTX-treated group, the transcript levels of hand2, mef2a, mef2c, and flk-1 were increased in the MTX + CF group [4]. Folinic Acid Calcium Pentahydrate may also be useful in the treatment of acute methotrexate overdose [3].

Folinic acid calcium salt pentahydrate 动物研究

Dose Mice: 7 mg/kg[3] (i.p.)
Administration i.p.

Folinic acid calcium salt pentahydrate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00720109 Adult B Acute Lymphoblastic Le... 展开 >>ukemia With t(9;22)(q34;q11.2); BCR-ABL1 Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia 收起 << Phase 2 Phase 3 Completed - -
NCT01256398 Acute Lymphoblastic Leukemia ... 展开 >> Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia 收起 << Phase 2 Active, not recruiting - -
NCT00720109 - Completed - -

Folinic acid calcium salt pentahydrate 参考文献

[1]Correale P, Cusi MG, et al. Dendritic cell-mediated cross-presentation of antigens derived from colon carcinoma cells exposed to a highly cytotoxic multidrug regimen with gemcitabine, oxaliplatin, 5-fluorouracil, and leucovorin, elicits a powerful human antigen-specific CTL response with antitumor activity in vitro. J Immunol. 2005 Jul 15;175(2):820-8.

[2]Van der Wilt CL, Pinedo HM, et al. Elevation of thymidylate synthase following 5-fluorouracil treatment is prevented by the addition of leucovorin in murine colon tumors. Cancer Res. 1992 Sep 15;52(18):4922-8.

[3] Calcium leucovorin - folinic acid rescue. Drug Ther Bull. 1978 Feb 3;16(3):11-2.

[4]Sun S, Gui Y, Wang Y, Qian L, Liu X, Jiang Q, Song H. Effects of methotrexate on the developments of heart and vessel in zebrafish. Acta Biochim Biophys Sin (Shanghai). 2009 Jan;41(1):86-96. doi: 10.1093/abbs/gmn010.

Folinic acid calcium salt pentahydrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.31mL

1.66mL

0.83mL

16.62mL

3.32mL

1.66mL

Folinic acid calcium salt pentahydrate 技术信息

CAS号6035-45-6
分子式C20H31CaN7O12
分子量 601.578
别名 亚叶酸钙五水合物 ;Leucovorin Calcium Pentahydrate;Leucovorin calcium salt pentahydrate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

H2O: 10 mg/mL(16.62 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 80 mg/mL clear

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