Cat. No.: HY-127009

Levoleucovorin

(Synonyms: Levofolinic acid; Levofolene)

Customer Review

Based on 1 Customer Validation

Levoleucovorin (Levofolinic acid; Levofolene) is the pharmacologically and orally active levoisomer of Folinic acid (HY-17556), a synthetic folate analogue. Levoleucovorin can inhibit LOXL2 with an IC₅₀ of 68.81 μM. Levoleucovorin can inhibit cancer cells proliferation, migration and induce apoptosis. Levoleucovorin can be used as a rescue agent for high-dose Methotrexate (HY-14519). Levoleucovorin can reduce the frequency of embryonic malformations. Levoleucovorin can be used for the research of can and endocrinology, such as breast cancer and osteosarcoma.

For research use only. We do not sell to patients.

Purity: 98.53%
CAS No.: 68538-85-2
Formula: C₂₀H₂₃N₇O₇
Molecular Weight:473.44

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Levoleucovorin Chemical Structure

CAS No.: 68538-85-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

LOXL2

68.81 nM (IC₅₀)

In Vitro

Levoleucovorin inhibits recombinant human LOXL2 protein with an IC₅₀ of 68.81 μM^[1].
Levoleucovorin (72 h) inhibits proliferation of MDA-MB 231 breast cancer cells with a GI₅₀ of 55.91 μM and MCF-7 breast cancer cells with a GI₅₀ of 79.20 μM^[1].
Levoleucovorin (15-60 μM; 12 h) dose-dependently inhibits HGF-induced trans-endothelial migration of MDA-MB 231 and MCF-7 breast cancer cells across HUVEC cell layers^[1].
Levoleucovorin (30-80 μM；72 h) induces dose-dependent apoptosis in MDA-MB 231 and MCF-7 breast cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB 231 breast cancer cell line, MCF-7 breast cancer cell line
Concentration:

30 μM, 60 μM (MDA-MB 231); 40 μM, 80 μM (MCF-7)
Incubation Time:

72 h
Result:

Significantly increased Annexin V-positive early and late apoptotic populations in MDA-MB 231 cells in a dose-dependent manner, with total apoptosis increasing 17.93% at 30 μM and 33.11% at 60 μM.
Significantly increased Annexin V-positive early and late apoptotic populations in MCF-7 cells in a dose-dependent manner, with total apoptosis increasing 15.36% at 40 μM and 30.38% at 80 μM.

In Vivo

Levoleucovorin (10.75-43 μmol/kg per day; i.g.,; daily; initiated 2 weeks pre-mating through gestation) reduces the frequency of embryonic malformations in a dose-dependent manner, with the 43 μmol/kg per day dose lowering overall malformation frequency to 33.3%^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Folbp1 knockout (female; mated to Folbp1-/- males; prenatal developmental model)^[3]
Dosage:

10.75 μmol/kg per day; 21.5 μmol/kg per day; 43 μmol/kg per day
Administration:

I.g.; daily; initiated 2 weeks pre-mating through gestation
Result:

Reduced malformation frequency to 66.7% at 10.75 μmol/kg per day, 65.8% at 21.5 μmol/kg per day, and 33.3% at 43 μmol/kg per day.
Decreased neural tube defects to 35.2% (10.75 and 21.5 μmol/kg), 16.7% (43 μmol/kg).
Decreased craniofacial defects to 46.2% (10.75 and 21.5 μmol/kg), 19.4% (43 μmol/kg).
Demonstrated significant inverse dose-dependent relationship with all malformation categories.
Resulted in a mean litter size of 3.70 ± 2.63 at 43 μmol/kg per day, significantly lower than wild-type controls.

Chemical Information

CAS No. 68538-85-2
Appearance Solid
Molecular Weight 473.44
Formula C₂₀H₂₃N₇O₇
Color Off-white to light yellow
SMILES

O=CN1C2=C(NC(N)=NC2=O)NC[C@@H]1CNC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCC(O)=O)=O
Synonyms

Levofolinic acid; Levofolene
Initial Source
- Endogenous metabolite
- Human Gut Microbiota Metabolites
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 35 mg/mL (73.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (70.40 mM; ultrasonic and adjust pH to 11 with 1 M NaOH)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1122 mL

10.5610 mL

21.1220 mL

5 mM

0.4224 mL

2.1122 mL

4.2244 mL

10 mM

0.2112 mL

1.0561 mL

2.1122 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deshpande H, et al. Levoleucovorin inhibits LOXL2 (lysyl oxidase like-2) to control breast cancer proliferation: a repurposing approach. J Biomol Struct Dyn. 2024;42(10):5104-5113. [Content Brief]

[2]. Chuang VT, et al. Levoleucovorin as replacement for leucovorin in cancer treatment. Ann Pharmacother. 2012;46(10):1349-1357. [Content Brief]

[3]. Spiegelstein O, et al. Embryonic development of folate binding protein-1 (Folbp1) knockout mice: Effects of the chemical form, dose, and timing of maternal folate supplementation. Dev Dyn. 2004;231(1):221-231. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.1122 mL	10.5610 mL	21.1220 mL	52.8050 mL
	5 mM	0.4224 mL	2.1122 mL	4.2244 mL	10.5610 mL
	10 mM	0.2112 mL	1.0561 mL	2.1122 mL	5.2805 mL
	15 mM	0.1408 mL	0.7041 mL	1.4081 mL	3.5203 mL
	20 mM	0.1056 mL	0.5281 mL	1.0561 mL	2.6403 mL
	25 mM	0.0845 mL	0.4224 mL	0.8449 mL	2.1122 mL
	30 mM	0.0704 mL	0.3520 mL	0.7041 mL	1.7602 mL
	40 mM	0.0528 mL	0.2640 mL	0.5281 mL	1.3201 mL
	50 mM	0.0422 mL	0.2112 mL	0.4224 mL	1.0561 mL
	60 mM	0.0352 mL	0.1760 mL	0.3520 mL	0.8801 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Levoleucovorin

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Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Levoleucovorin Related Classifications

HY-127009 Related Classifications