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