Art. -Nr.: HY-101943

LY 345899

Name: LY 345899
Brand: MedChemExpress
SKU: HY-101943
Price: 200.00 USD
Availability: InStock
Rating: 5 (9 reviews)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC₅₀ values of 96 nM and 663 nM, respectively and a K_i of 18 nM for MTHFD1.

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Reinheit : 98.0%
CAS. Nr.: 10538-99-5
Formel: C₂₀H₂₁N₇O₇
Molecular Weight:471.42

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year

LY 345899 Chemical Structure

CAS. Nr.: 10538-99-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Ki: 18 nM (MTHFD1)^[1]; IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)^[3]

In Vitro

LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria^[4].
LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis^[4].

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

In Vivo

LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo^[1].

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

Animal Model:

SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model^[4]
Dosage:

5-10 mg/kg
Administration:

Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks
Result:

Displayed lower cell proliferation indices and higher cell apoptosis.
Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice.

Chemical Information

CAS. Nr. 10538-99-5
Appearance Solid
Molecular Weight 471.42
Formel C₂₀H₂₁N₇O₇
Color Light yellow to yellow
SMILES

O=C(O)[C@@H](NC(C1=CC=C(N2C(N3C4=C(NC(N)=NC4=O)NCC3C2)=O)C=C1)=O)CCC(O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

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Journal Impact Factor

Cancer Res

MTHFD2 Enhances cMYC O-GlcNAcylation to Promote Sunitinib Resistance in Renal Cell Carcinoma. [Abstract]

2025 Mar 14;85(6):1113-1129. PMID: 39804969
Nat Commun

Non-canonical dihydrolipoyl transacetylase promotes chemotherapy resistance via mitochondrial tetrahydrofolate signaling. [Abstract]

2025 Oct 8;16(1):8932. PMID: 41062483
Phytomedicine

Effect of isoginkgetin on targeting methylenetetrahydrofolate dehydrogenase 2 to induce ROS-mediated apoptosis in non-small cell lung cancer. [Abstract]

2026 Jun 16:159:158425. PMID: 42361761
Cancers (Basel)

Cysteine and Folate Metabolism Are Targetable Vulnerabilities of Metastatic Colorectal Cancer. [Abstract]

2021 Jan 23;13(3):425. PMID: 33498690
J Biol Chem

Mitochondrial folate metabolism-mediated α-linolenic acid exhaustion masks liver fibrosis resolution. [Abstract]

2023 Jul;299(7):104909. PMID: 37307917
bioRxiv

Formate reduces ischemic injury in female hearts lacking alcohol dehydrogenase 5. [Abstract]

2025 Aug 1:2025.07.29.667470. PMID: 40766369
Res Sq

2025 Jul 18.
Biomed Pharmacother

Pharmacological targeting of MTHFD2 suppresses NSCLC via the regulation of ILK signaling pathway. [Abstract]

2023 May:161:114412. PMID: 36827714
bioRxiv

2021 Feb 3.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (265.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.1213 mL

10.6063 mL

21.2125 mL

5 mM

0.4243 mL

2.1213 mL

4.2425 mL

10 mM

0.2121 mL

1.0606 mL

2.1213 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)

Verweise

[1]. Schmidt A, et al. Structures of three inhibitor complexes provide insight into the reaction mechanism of the human methylenetetrahydrofolate dehydrogenase/cyclohydrolase. Biochemistry. 2000 May 30;39(21):6325-35. [Content Brief]

[2]. Tedeschi PM, et al. Mitochondrial Methylenetetrahydrofolate Dehydrogenase (MTHFD2) Overexpression Is Associated with Tumor Cell Proliferation and Is a Novel Target for Drug Development. Mol Cancer Res. 2015 Oct;13(10):1361-6. [Content Brief]

[3]. Gustafsson R, et al. Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor. Cancer Res. 2017 Feb 15;77(4):937-948. [Content Brief]

[4]. Huai-Qiang Ju, et al.Modulation of Redox Homeostasis by Inhibition of MTHFD2 in Colorectal Cancer: Mechanisms and Therapeutic Implications. J Natl Cancer Inst. 2019 Jun 1;111(6):584-596. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1213 mL	10.6063 mL	21.2125 mL	53.0313 mL
	5 mM	0.4243 mL	2.1213 mL	4.2425 mL	10.6063 mL
	10 mM	0.2121 mL	1.0606 mL	2.1213 mL	5.3031 mL
	15 mM	0.1414 mL	0.7071 mL	1.4142 mL	3.5354 mL
	20 mM	0.1061 mL	0.5303 mL	1.0606 mL	2.6516 mL
	25 mM	0.0849 mL	0.4243 mL	0.8485 mL	2.1213 mL
	30 mM	0.0707 mL	0.3535 mL	0.7071 mL	1.7677 mL
	40 mM	0.0530 mL	0.2652 mL	0.5303 mL	1.3258 mL
	50 mM	0.0424 mL	0.2121 mL	0.4243 mL	1.0606 mL
	60 mM	0.0354 mL	0.1768 mL	0.3535 mL	0.8839 mL
	80 mM	0.0265 mL	0.1326 mL	0.2652 mL	0.6629 mL
	100 mM	0.0212 mL	0.1061 mL	0.2121 mL	0.5303 mL

Bioz

Keywords

LY 345899

9 Cited Publications

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LY 345899

Publications Citing Use of MedChemExpress (MCE) LY 345899