Cat. No.: HY-130251

DS18561882

21 Cited Publications

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Based on 21 publication(s) in Google Scholar

DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC₅₀ value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC₅₀=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.

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Pureté: 99.95%
CAS No.: 2227149-22-4
Formule: C₂₈H₃₁F₃N₄O₆S
Masse moléculaire:608.63

Stockage:

4°C, stored under nitrogen

* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

DS18561882 Chemical Structure

CAS No.: 2227149-22-4

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (21)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 0.0063 μM (MTHFD2); 0.57 μM (MTHFD1)^[1]

In Vitro

DS18561882 (0-150 nM) gives the lowest GI₅₀ value (140 nM) against the MDA-MB-231 cell line^[1].

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

In Vivo

DS18561882 (oral administration; 30, 100 or 300 mg/kg; twice daily) inhibits tumor growth inhibition with a dose-dependent manner, the tumor is completely inhibited (TGI: 67%) at the dose of 300 mg/kg in mice^[1].
DS18561882 (oral administration; 10, 30, 100, or 300 mg/kg) has a good oral pharmacokinetic profile, including ACU (64.6, 264, 726 μg.h/ml ); C_max (11.4, 56.5, 90.1 μg/ml); t_1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively^[1].
DS18561882 is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article^[1].

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

Animal Model:

Five week old female BALB/cAJcl-nu/nu mice with MDA-MB-231 luc tumor cells (4 × 10⁶ cells/mouse)^[1]
Dosage:

30, 100 or 300 mg/kg
Administration:

Oral administration; 30, 100 or 300 mg/kg; twice daily; until day 11
Result:

Suppressed tumor growth in a dose-dependent manner.

Chemical Information

CAS No. 2227149-22-4
Appearance Solid
Masse moléculaire 608.63
Formule C₂₈H₃₁F₃N₄O₆S
Color White to yellow
SMILES

CS(=O)(NC1=CC=C(C(N2CCC(C3=CC=C(N4C[C@H](C)N(C)CC4)C(C)=C3O5)=C(C5=O)C2)=O)C=C1OC(F)(F)F)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

Publications (21)

All 2D/3D Cell Culture and DifferentiationWBCell Proliferation/Viability AssayHistological Imaging/StainingApoptosis Analysis

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Journal Impact Factor

Nat Metab

Metabolic collateral lethal target identification reveals MTHFD2 paralogue dependency in ovarian cancer. [Abstract]

2022 Sep;4(9):1119-1137. PMID: 36131208
Cell Stem Cell

Mitochondrial serine catabolism safeguards maintenance of the hematopoietic stem cell pool in homeostasis and injury. [Abstract]

2024 Aug 21:S1934-5909(24)00285-6. PMID: 39181130

DS18561882 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2024 Aug 21:S1934-5909(24)00285-6. [Abstract]

HSC numbers per well following HSC culture in CM or SGFM supplemented with or without DS18561882 (50 μM; 10 days) (n = 3).

DS18561882 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2024 Aug 21:S1934-5909(24)00285-6. [Abstract]

Ferroptosis susceptibility analysis of HSCs following culture in CM or SGFM supplemented with or without DS18561882 (50 μM; 10 days) (n = 3).
Nat Commun

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

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

DS18561882 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Oct 8;16(1):8932. [Abstract]

Effect of MTHFD2 inhibitors on cisplatin-mediated apoptotic cell death. Cells were treated with either 10 μM DS18561882 and sublethal doses of cisplatin for 48 h.

DS18561882 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Oct 8;16(1):8932. [Abstract]

Effect of MTHFD2 inhibitors on cisplatin-mediated cell viability. Cells were treated with either 10 μM DS18561882 and sublethal doses of cisplatin for 48 h.
Nat Commun

Mitochondrial one-carbon metabolism is required for TGF-β-induced glycine synthesis and fibrotic responses. [Abstract]

2025 Oct 20;16(1):9250. PMID: 41115888

DS18561882 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Oct 20;16(1):9250. [Abstract]

Western blot analysis of collagen and α-smooth muscle actin protein expression in human lung fibroblasts (HLFs) treated with TGF-β for the indicated intervals in the presence or absence of DS18561882 (5 μM; 24-48 h).

DS18561882 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Oct 20;16(1):9250. [Abstract]

Histological analysis of mouse lung tissue from DS18561882 (100 mg/kg; i.p.) or vehicle treated mice on Day 21 after bleomycin instillation. The results showed that DS18561882 significantly alleviated the degree of pulmonary fibrosis in mice.
Redox Biol

Regulation of redox homeostasis by ATF4-MTHFD2 axis during white adipose tissue browning. [Abstract]

2025 Jun 9:85:103715. PMID: 40516456
J Exp Clin Cancer Res

PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2. [Abstract]

2022 Apr 5;41(1):125. PMID: 35382861
Cell Death Dis

SOX4-STAT6-MTHFD2 axis drives hepatocellular carcinoma progression and treatment resistance. [Abstract]

2026 Jan 3. PMID: 41484064
Cancer Lett

Folate enzyme MTHFD2 links one-carbon metabolism to unfolded protein response in glioblastoma. [Abstract]

2022 Nov 28:549:215903. PMID: 36089117
Cell Death Discov

Targeting mitochondrial one-carbon enzyme MTHFD2 together with pemetrexed confers therapeutic advantages in lung adenocarcinoma. [Abstract]

2022 Jul 5;8(1):307. PMID: 35790743
Int J Biol Macromol

Methylenetetrahydrofolate dehydrogenase 2 promotes cutaneous squamous cell carcinoma progression by reprogramming metabolism and interacting with fatty acid synthase. [Abstract]

2026 Feb:345:150486. PMID: 41579995
BMC Med

MTHFD2 promotes osteoclastogenesis and bone loss in rheumatoid arthritis by enhancing CKMT1-mediated oxidative phosphorylation. [Abstract]

2025 Feb 27;23(1):124. PMID: 40016725
Int J Mol Sci

Integration of Bulk and Single-Cell Transcriptomics Reveals Prognostic and Immunological Roles of MTHFD2 in Clear Cell Renal Cell Carcinoma. [Abstract]

2026 Feb 20;27(4):2021. PMID: 41752156
Oncol Res

UHMK1 Promotes Prostate Cancer Progression through a Positive Feedback Loop with MTHFD2. [Abstract]

2025 Aug 28;33(9):2331-2351. PMID: 40918462
Metabolites

Regulation and Therapeutic Targeting of MTHFD2 and EZH2 in KRAS-Mutated Human Pulmonary Adenocarcinoma. [Abstract]

2022 Jul 15;12(7):652. PMID: 35888776
Magn Reson Med

Deuterium MRI of serine metabolism in mouse models of glioblastoma. [Abstract]

2024 Nov;92(5):1811-1821. PMID: 38946234
Res Sq

2026 Mar 5.
bioRxiv

2025 July 11.
bioRxiv

Inhibition of formate production blocks CD8 + T-cell responses and delays disease onset in a mouse model of type 1 diabetes. [Abstract]

2025 Jul 8:2025.07.04.663229. PMID: 40672325
Research Square Preprint

2024 Apr 5.
Research Square Preprint

2023 Mar 29.
bioRxiv

2021 Feb 3.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (164.30 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

1.6430 mL

8.2152 mL

16.4303 mL

5 mM

0.3286 mL

1.6430 mL

3.2861 mL

10 mM

0.1643 mL

0.8215 mL

1.6430 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 (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.11 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

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

Solubility: 2.5 mg/mL (4.11 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: 2.5 mg/mL (4.11 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. Kawai J, et al. Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with In Vivo Anti-Tumor Activity. J Med Chem. 2019 Oct 22. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6430 mL	8.2152 mL	16.4303 mL	41.0759 mL
	5 mM	0.3286 mL	1.6430 mL	3.2861 mL	8.2152 mL
	10 mM	0.1643 mL	0.8215 mL	1.6430 mL	4.1076 mL
	15 mM	0.1095 mL	0.5477 mL	1.0954 mL	2.7384 mL
	20 mM	0.0822 mL	0.4108 mL	0.8215 mL	2.0538 mL
	25 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6430 mL
	30 mM	0.0548 mL	0.2738 mL	0.5477 mL	1.3692 mL
	40 mM	0.0411 mL	0.2054 mL	0.4108 mL	1.0269 mL
	50 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8215 mL
	60 mM	0.0274 mL	0.1369 mL	0.2738 mL	0.6846 mL
	80 mM	0.0205 mL	0.1027 mL	0.2054 mL	0.5134 mL
	100 mM	0.0164 mL	0.0822 mL	0.1643 mL	0.4108 mL

Keywords

DS18561882

21 Cited Publications

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DS18561882

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) DS18561882

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

DS18561882

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) DS18561882

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

DS18561882 Related Classifications

HY-130251 Related Classifications