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DS18561882

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TargetMol
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.

DS18561882

DS18561882

🥰Excellent
TargetMol
Purity: 99.63%
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.
Pack SizePriceAvailabilityQuantity
1 mg$117In Stock
5 mg$289In Stock
10 mg$455In Stock
25 mg$818In Stock
50 mg$1,330In Stock
100 mg$1,790In Stock
1 mL x 10 mM (in DMSO)$397In Stock
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Purity:99.63%
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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
MTHFD1:0.57 μM, MTHFD2:0.0063 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 Weight608.63
FormulaC28H31F3N4O6S
Cas No.2227149-22-4
SmilesC[C@H]1CN(CCN1C)c1ccc2c3CCN(Cc3c(=O)oc2c1C)C(=O)c1ccc(NS(C)(=O)=O)c(OC(F)(F)F)c1
Relative Density.1.47 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (131.44 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6430 mL8.2152 mL16.4303 mL82.1517 mL
5 mM0.3286 mL1.6430 mL3.2861 mL16.4303 mL
10 mM0.1643 mL0.8215 mL1.6430 mL8.2152 mL
20 mM0.0822 mL0.4108 mL0.8215 mL4.1076 mL
50 mM0.0329 mL0.1643 mL0.3286 mL1.6430 mL
100 mM0.0164 mL0.0822 mL0.1643 mL0.8215 mL

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