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DS18561882

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Purity:99.63%

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COA HNMR HPLC LCMS

DS18561882

Catalog No. T11103Cas No. 2227149-22-4

DS18561882 is an orally available, selective and potent inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) with antitumor activity, inhibits MTHFD1 activity and can be used in the study of breast cancer.

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Pack Size	Price	Availability
1 mg	$117	In Stock
5 mg	$289	In Stock
10 mg	$455	In Stock
25 mg	$818	In Stock
50 mg	$1,330	In Stock
100 mg	$1,790	In Stock
1 mL x 10 mM (in DMSO)	$397	In Stock

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Product Introduction

Bioactivity

Description	DS18561882 is an orally available, selective and potent inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) with antitumor activity, inhibits MTHFD1 activity and can be used in the study of breast cancer.
Targets&IC50	MTHFD2:0.0063 μM, MTHFD1:0.57 μM
In vitro	DS18561882 (0-150 nM) achieves the lowest GI50 value (140 nM) against the MDA-MB-231 cell line.
In vivo	DS18561882 (oral; 10mg/kg, 30mg/kg, 100mg/kg or 300mg/kg) has good oral pharmacokinetics, including ACU (64.6, 264, 726ug.H/ml); Cmax (11.4, 56.5, 90.1° g)/ml). T1/2 (2.21, 2.16, 2.32 hours) are 30 mg/kg; 100 mg/kg; 200 mg/kg respectively. DS18561882 was suspended in 0.5% (W/V) methylcellulose 400 solution. DS18561882 (oral; 30, 100 or 300 mg/kg); tumor growth inhibition was inhibited in a dose-dependent manner and was completely inhibited at 300 mg/kg in mice (TGI: 67%).[1]

Chemical Properties

Molecular Weight	608.63
Formula	C28H31F3N4O6S
Cas No.	2227149-22-4

Storage & Solubility Information

Storage

Solubility Information

DMSO: 80 mg/mL (131.44 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6430 mL	8.2152 mL	16.4303 mL	82.1517 mL
5 mM	0.3286 mL	1.6430 mL	3.2861 mL	16.4303 mL
10 mM	0.1643 mL	0.8215 mL	1.6430 mL	8.2152 mL
20 mM	0.0822 mL	0.4108 mL	0.8215 mL	4.1076 mL
50 mM	0.0329 mL	0.1643 mL	0.3286 mL	1.6430 mL
100 mM	0.0164 mL	0.0822 mL	0.1643 mL	0.8215 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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