Art. -Nr.: HY-100184

DSM265

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC₅₀ of 4.3 nM.

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Reinheit: 99.92%
CAS. Nr.: 1282041-94-4
Formel: C₁₄H₁₂F₇N₅S
Molecular Weight:415.33

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DSM265 Chemical Structure

CAS. Nr.: 1282041-94-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Plasmodium

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	>30 μM Compound: DSM265	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 33620219]
HepG2	CC₅₀	>50 μM Compound: 1; DSM265	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability Cytotoxicity against human HepG2 cells assessed as reduction in cell viability	[PMID: 32248693]
HepG2	EC₅₀	>50 μM Compound: 38, DSM265	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 21696174]
L1210	CC₅₀	>50 μM Compound: 1; DSM265	Cytotoxicity against mouse L1210 cells assessed as reduction in cell viability Cytotoxicity against mouse L1210 cells assessed as reduction in cell viability	[PMID: 32248693]
L1210	EC₅₀	>50 μM Compound: 38, DSM265	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 21696174]

In Vivo

DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD-scid IL-2Rγnull (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose (ED₉₀) of 3 mg/kg per day (1.5 mg/kg twice daily). The maximum rate of parasite killing occurred at and above a dose of 13 mg/kg per day (6.4 mg/kg twice daily).
DSM265 has moderate terminal elimination half-life (t_1/2) of 2-4 hours for mice (0.5 to 75 mg/kg, oral) ^[2].

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

Animal Model:

NOD-scid IL-2Rγnull (NSG) mice (23-36 g)^[2]
Dosage:

0.5 to 75 mg/kg
Administration:

Oral administration; twice daily; for 4 days
Result:

Had potent antimalarial activity with 90% effective dose (ED₉₀) of 3 mg/kg per day (1.5 mg/kg twice daily).

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1282041-94-4
Appearance Solid
Molecular Weight 415.33
Formel C₁₄H₁₂F₇N₅S
Color White to off-white
SMILES

CC1=NC2=NC(C(C)(F)F)=NN2C(NC3=CC=C(S(F)(F)(F)(F)F)C=C3)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Travel Med Infect Dis

Artemisinin resistance-associated gene mutations in Plasmodium falciparum: A case study of severe malaria from Mozambique. [Abstract]

2024 Jan-Feb:57:102684. PMID: 38159875
ACS Infect Dis

Integral Solvent-Induced Protein Precipitation for Target-Engagement Studies in Plasmodium falciparum. [Abstract]

2024 Dec 13;10(12):4073-4086. PMID: 39631773

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (120.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 11.11 mg/mL (26.75 mM; Need ultrasonic)

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

2.4077 mL

12.0386 mL

24.0772 mL

5 mM

0.4815 mL

2.4077 mL

4.8154 mL

10 mM

0.2408 mL

1.2039 mL

2.4077 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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% Corn Oil

Solubility: ≥ 2.75 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 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 (285 KB)
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 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]. Kokkonda S, et al. Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparumDihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity. J Med Chem. 2016 Jun 9;59(11):5416-31. [Content Brief]

[2]. Phillips MA, et al. A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Sci Transl Med. 2015 Jul 15;7(296):296ra111. [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
Ethanol / DMSO	1 mM	2.4077 mL	12.0386 mL	24.0772 mL	60.1931 mL
	5 mM	0.4815 mL	2.4077 mL	4.8154 mL	12.0386 mL
	10 mM	0.2408 mL	1.2039 mL	2.4077 mL	6.0193 mL
	15 mM	0.1605 mL	0.8026 mL	1.6051 mL	4.0129 mL
	20 mM	0.1204 mL	0.6019 mL	1.2039 mL	3.0097 mL
	25 mM	0.0963 mL	0.4815 mL	0.9631 mL	2.4077 mL
DMSO	30 mM	0.0803 mL	0.4013 mL	0.8026 mL	2.0064 mL
	40 mM	0.0602 mL	0.3010 mL	0.6019 mL	1.5048 mL
	50 mM	0.0482 mL	0.2408 mL	0.4815 mL	1.2039 mL
	60 mM	0.0401 mL	0.2006 mL	0.4013 mL	1.0032 mL
	80 mM	0.0301 mL	0.1505 mL	0.3010 mL	0.7524 mL
	100 mM	0.0241 mL	0.1204 mL	0.2408 mL	0.6019 mL

Keywords

DSM265

2 Cited Publications

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DSM265

Vidofludimus

Brequinar

Farudodstat

ML390

JNJ-74856665

AG-636

DHODH-IN-1

hDHODH-IN-4

hDHODH-IN-3

DHODH-IN-14

hDHODH-IN-5

BAY-2402234

Publications Citing Use of MedChemExpress (MCE) DSM265

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DSM265

Vidofludimus

Brequinar

Farudodstat

ML390

JNJ-74856665

AG-636

DHODH-IN-1

hDHODH-IN-4

hDHODH-IN-3

DHODH-IN-14

hDHODH-IN-5

BAY-2402234

Publications Citing Use of MedChemExpress (MCE) DSM265

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DSM265 Related Classifications

HY-100184 Related Classifications