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Leucovorin (Folinic acid) Calcium Pentahydrate DHFR chemical

Cat.No.S1236

Leucovorin (Folinic acid) Calcium Pentahydrate is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.Solutions are unstable and should be fresh-prepared.
Leucovorin (Folinic acid) Calcium Pentahydrate DHFR chemical Chemical Structure

Chemical Structure

Molecular Weight: 601.58

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Chemical Information, Storage & Stability

Molecular Weight 601.58 Formula

C20H31CaN7O12

 Storage (From the date of receipt) 4°C (in the dark)
CAS No. 6035-45-6 Download SDF Storage of Stock Solutions Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.
Synonyms NSC-3590 Calcium Pentahydrate, Calcium Folinatc, Citrovorum Factor Smiles C1C(N(C2=C(N1)N=C(NC2=O)N)C=O)CNC3=CC=C(C=C3)C(=O)NC(CCC(=O)[O-])C(=O)[O-].O.O.O.O.O.[Ca+2]

Solubility

In vitro
Batch:

Water : 10 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
thymidylate synthase [1]
In vitro

Leucovorin administration increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase in two murine colon tumors. [1] 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. [2] Leucovorin (20 mM) increases the cytotoxicity in all three replicate experiments in 10 of the 11 human colorectal carcinoma cell lines. [3] Leucovorin enhances cytotoxicity of trimetrexate/fluorouracil, but not methotrexate/fluorouracil, in CCRF-CEM cells. [4] 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. [5]
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. [5] 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. [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/1376779/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10999757/
  • [6] https://pubmed.ncbi.nlm.nih.gov/9506532/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06403189 Not yet recruiting
Plexus Choroideus|Metabolic Syndrome
Assistance Publique - Hôpitaux de Paris
 July 1 2024 Not Applicable
NCT05013164 Completed
Autism Spectrum Disorder
Nishtar Medical University
 October 1 2020 Phase 2
NCT04060030 Recruiting
Autism Spectrum Disorder|Language Disorders
Southwest Autism Research & Resource Center|Autism Speaks|State University of New York - Downstate Medical Center
 October 8 2020 Phase 2
NCT04060017 Recruiting
Autism Spectrum Disorder|Language Disorders
Southwest Autism Research & Resource Center|State University of New York - Downstate Medical Center|United States Department of Defense
 September 22 2020 Phase 2

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