Leucovorin Calcium - 半岛电竞官方网址

Molecular Weight (MW)	601.58
Formula	C21H25CaN7O7.5H2O
CAS No.	6035-45-6
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility(In vitro)	DMSO: <1 mg/mL
Water: 40 mg/mL (66.5 mM)
Ethanol: <1 mg/mL
Other info	Chemical Name: L-Glutamic acid, N-(4-(((2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl)amino)benzoyl)-, calcium salt (1:1), pentahydrate InChi Key: NPPBLUASYYNAIG-ZIGBGYJWSA-L InChi Code: InChI=1S/C20H23N7O7.Ca.5H2O/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30;;;;;;/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32);;5*1H2/q;+2;;;;;/p-2/t12?,13-;;;;;;/m0....../s1 SMILES Code: O=C([O-])CC[C@@H](C([O-])=O)NC(C1=CC=C(NCC2N(C=O)C3=C(NC(N)=NC3=O)NC2)C=C1)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Ca+2]
Synonyms	Folinic acid; Folinic acid calcium salt pentahydrate; Leucovorin calcium hydrate; Leucovorin Calcium; Calcium Folinate

Molecular Weight (MW)

601.58

Formula

C21H25CaN7O7.5H2O

CAS No.

6035-45-6

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility(In vitro)

DMSO: <1 mg/mL

Water: 40 mg/mL (66.5 mM)

Ethanol: <1 mg/mL

Other info

Chemical Name: L-Glutamic acid, N-(4-(((2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl)amino)benzoyl)-, calcium salt (1:1), pentahydrate
InChi Key: NPPBLUASYYNAIG-ZIGBGYJWSA-L
InChi Code: InChI=1S/C20H23N7O7.Ca.5H2O/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30;;;;;;/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32);;5*1H2/q;+2;;;;;/p-2/t12?,13-;;;;;;/m0....../s1
SMILES Code: O=C([O-])CC[C@@H](C([O-])=O)NC(C1=CC=C(NCC2N(C=O)C3=C(NC(N)=NC3=O)NC2)C=C1)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Ca+2]

Synonyms

Folinic acid; Folinic acid calcium salt pentahydrate; Leucovorin calcium hydrate; Leucovorin Calcium; Calcium Folinate

In Vitro	In vitroactivity: Leucovorin administration increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase in two murine colon tumors. Leucovorin, Gemcitabine, Oxaliplatin, and 5-fluorouracil is a powerful antitumor and immunomodulating regimen that can make the tumor cells a suitable means to induce an Ag-specific CTL response. Leucovorin (20 mM) increases the cytotoxicity in all three replicate experiments in 10 of the 11 human colorectal carcinoma cell lines. Leucovorin enhances cytotoxicity of trimetrexate/fluorouracil, but not methotrexate/fluorouracil, in CCRF-CEM cells. Leucovorin (LV) is a reduced folate cofactor that competes with RTX for transport and polyglutamation in both tumor and normal tissues and thus has potential as a rescue agent. Leucovorin reverses the growth-inhibitory, and potentially cytotoxic, effects of RTX on populations of viable cells. Cell Assay: Increasing concentrations of leucovorin (N5-CHO-THF) inhibit both zcSHMT and hcSHMT activities substantially, yet to a lesser extent than zmSHMT. The IC50 of leucovorin is approximately 30 μM for zcSHMT and higher than 70 μM for zmSHMT. The differential inhibition is evident with the presence of 10 μM leucovorin, the concentration estimated in serum in a high-dose leucovorin rescue regimen .
In Vivo	Leucovorin (200 mg/kg), which is given after the onset of severe weight loss and diarrhea (twice daily, days 5-7) in mice, prevents further weight loss and induces earlier recovery. Leucovorin (100 or 200 mg/kg; twice daily on days 4-6) reduces the RTX concentration in the liver 2-4-fold on days 7, 9, and 11 compared with controls. Leucovorin/5-FU and Gastrimmune (200 mg/mL) combinations (12.5 and 20 mg/kg) increase the therapeutic effects on the in vivo growth of DHDK12 tumors when compared to the agents given singly.
Animal model	Clinical trial
Formulation & Dosage	Following intravenous administration, peak plasma concentrations of (6R) LV, (6S) LV, and 5-CH3 THF were 148 +/- 32, 59.1 +/- 22, and 17.8 +/- 17 microM, respectively. During oral administration of LV, virtually no (6S) LV appeared in the plasma. Steady-state plasma concentrations of (6R) LV and 5-CH3 THF were approximately 1.5 +/- 0.23 and 2.8 +/- 0.41 microM, respectively. 24 fasted subjects were given 4 of a series of 5 single test doses between 20 and 100 mg, at 1-week intervals, of 5-formyl-THF as an oral solution of leucovorin calcium. Six separate subjects received 200 mg iv and po in a 2-way crossover. Blood and urine samples were collected over 24 hours for differential microbiological folate assays using Lactobacillus casei and Streptococcus faecalis. Using L casei activity to measure total serum folates, the area under the concentration-time curve from 0 to infinite time (AUC[0-infinity]) was calculated. Relative bioavailabilities were 78%, 62%, 49%, and 42% for the 40-, 60-, 80-, and 100-mg doses, respectively. Clinical trial: Leucovorin and Fluorouracil With or Without SU-5416 in Treating Patients With Metastatic Colorectal Cancer
References	Cancer Res. 1992 Sep 15;52(18):4922-8; J Immunol. 2005 Jul 15;175(2):820-8; Clin Cancer Res. 2000 Sep;6(9):3646-56; Int J Cancer. 1998 Mar 16;75(6):873-7.

In Vitro

In vitroactivity: Leucovorin administration increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase in two murine colon tumors. Leucovorin, Gemcitabine, Oxaliplatin, and 5-fluorouracil is a powerful antitumor and immunomodulating regimen that can make the tumor cells a suitable means to induce an Ag-specific CTL response. Leucovorin (20 mM) increases the cytotoxicity in all three replicate experiments in 10 of the 11 human colorectal carcinoma cell lines. Leucovorin enhances cytotoxicity of trimetrexate/fluorouracil, but not methotrexate/fluorouracil, in CCRF-CEM cells. Leucovorin (LV) is a reduced folate cofactor that competes with RTX for transport and polyglutamation in both tumor and normal tissues and thus has potential as a rescue agent. Leucovorin reverses the growth-inhibitory, and potentially cytotoxic, effects of RTX on populations of viable cells.

Cell Assay: Increasing concentrations of leucovorin (N5-CHO-THF) inhibit both zcSHMT and hcSHMT activities substantially, yet to a lesser extent than zmSHMT. The IC50 of leucovorin is approximately 30 μM for zcSHMT and higher than 70 μM for zmSHMT. The differential inhibition is evident with the presence of 10 μM leucovorin, the concentration estimated in serum in a high-dose leucovorin rescue regimen .

In Vivo

Leucovorin (200 mg/kg), which is given after the onset of severe weight loss and diarrhea (twice daily, days 5-7) in mice, prevents further weight loss and induces earlier recovery. Leucovorin (100 or 200 mg/kg; twice daily on days 4-6) reduces the RTX concentration in the liver 2-4-fold on days 7, 9, and 11 compared with controls. Leucovorin/5-FU and Gastrimmune (200 mg/mL) combinations (12.5 and 20 mg/kg) increase the therapeutic effects on the in vivo growth of DHDK12 tumors when compared to the agents given singly.

Animal model

Clinical trial

Formulation & Dosage

Following intravenous administration, peak plasma concentrations of (6R) LV, (6S) LV, and 5-CH3 THF were 148 +/- 32, 59.1 +/- 22, and 17.8 +/- 17 microM, respectively. During oral administration of LV, virtually no (6S) LV appeared in the plasma. Steady-state plasma concentrations of (6R) LV and 5-CH3 THF were approximately 1.5 +/- 0.23 and 2.8 +/- 0.41 microM, respectively. 24 fasted subjects were given 4 of a series of 5 single test doses between 20 and 100 mg, at 1-week intervals, of 5-formyl-THF as an oral solution of leucovorin calcium. Six separate subjects received 200 mg iv and po in a 2-way crossover. Blood and urine samples were collected over 24 hours for differential microbiological folate assays using Lactobacillus casei and Streptococcus faecalis. Using L casei activity to measure total serum folates, the area under the concentration-time curve from 0 to infinite time (AUC[0-infinity]) was calculated. Relative bioavailabilities were 78%, 62%, 49%, and 42% for the 40-, 60-, 80-, and 100-mg doses, respectively. Clinical trial: Leucovorin and Fluorouracil With or Without SU-5416 in Treating Patients With Metastatic Colorectal Cancer

References

Cancer Res. 1992 Sep 15;52(18):4922-8; J Immunol. 2005 Jul 15;175(2):820-8; Clin Cancer Res. 2000 Sep;6(9):3646-56; Int J Cancer. 1998 Mar 16;75(6):873-7.

CAS NO:	6035-45-6
规格:	≥98%

包装	价格(元)
500mg	电议
1g	电议
2g	电议
5g	电议
10g	电议
25g	电议
50g	电议