Home Metabolism DHFR inhibitor Leucovorin Calcium Pentahydrate (Folinic acid)

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Leucovorin Calcium Pentahydrate (Folinic acid) DHFR Inhibitor

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 Calcium Pentahydrate (Folinic acid) DHFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 601.58

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Quality Control

Batch: Purity: 99.90%
99.90

Solubility

In vitro
Batch:

Water : 10 mg/mL

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

Ethanol : Insoluble

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In vivo
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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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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]

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Mechanism of Action

Targets/IC50/Ki
thymidylate synthase
In vitro

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.

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.

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 2026-06-18)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06365008 NOT_YET_RECRUITING
Unresectable/Metastatic Gastric Cancer
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University
 2026-06 PHASE2
NCT03959085 RECRUITING
B Acute Lymphoblastic Leukemia; B Lymphoblastic Lymphoma; Central Nervous System Leukemia; Mixed Phenotype Acute Leukemia; Testicular Leukemia
Children's Oncology Group
 2019-10-31 PHASE3
NCT06780111 RECRUITING
Esophageal Squamous Cell Carcinoma
Merck Sharp & Dohme LLC
 2025-07-30 PHASE1; PHASE2
NCT03801876 ACTIVE_NOT_RECRUITING
Clinical Stage I Esophageal Adenocarcinoma AJCC v8; Clinical Stage I Esophageal Squamous Cell Carcinoma AJCC v8; Clinical Stage I Gastroesophageal Junction Adenocarcinoma AJCC v8; Clinical Stage II Esophageal Adenocarcinoma AJCC v8; Clinical Stage II Esophageal Squamous Cell Carcinoma AJCC v8; Clinical Stage II Gastroesophageal Junction Adenocarcinoma AJCC v8; Clinical Stage III Esophageal Adenocarcinoma AJCC v8; Clinical Stage III Esophageal Squamous Cell Carcinoma AJCC v8; Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8; Clinical Stage IVA Esophageal Adenocarcinoma AJCC v8; Clinical Stage IVA Esophageal Squamous Cell Carcinoma AJCC v8; Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8; Thoracic Esophagus Squamous Cell Carcinoma
NRG Oncology
 2019-06-26 PHASE3
NCT07636564 NOT_YET_RECRUITING
Acute Leukemia of Ambiguous Lineage; B Acute Lymphoblastic Leukemia; B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative; T Acute Lymphoblastic Leukemia
SWOG Cancer Research Network
 2026-10-14 PHASE2
NCT07271355 NOT_YET_RECRUITING
Metastatic Appendix Carcinoma; Metastatic Colorectal Carcinoma; Metastatic Malignant Neoplasm in the Peritoneum; Stage IV Appendix Carcinoma AJCC v8; Stage IVC Colorectal Cancer AJCC v8; Unresectable Colorectal Carcinoma
City of Hope Medical Center
 2026-10-01 PHASE3

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