DS18561882

Name: DS18561882
Brand: MedChemExpress
SKU: HY-130251
Rating: 5.0 (21 reviews)

Cat. No.: HY-130251 Purity: 99.87%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 2227149-22-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 21 publication(s) in Google Scholar

21 Publications Citing Use of MCE DS18561882

2D/3D Cell Culture and Differentiation

Cell Proliferation/Viability Assay

Histological Imaging/Staining

Apoptosis Analysis

: 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 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 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.

: 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.

: 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).

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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.

Molecular Weight

608.63

Formula

C₂₈H₃₁F₃N₄O₆S

CAS No.

2227149-22-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (250 KB) RP-HPLC (219 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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

DS18561882 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DS185618822227149-22-4DS 18561882DS-18561882Methylenetetrahydrofolate Dehydrogenase (MTHFD)Inhibitorinhibitorinhibit

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DS18561882

Customer Review

DS18561882 Related Antibodies

21 Publications Citing Use of MCE DS18561882

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Complete Stock Solution Preparation Table

DS18561882 Related Classifications

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