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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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 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 |
| 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, MDA-MB-231 cells cell line:140 nM (GL50) |
| 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] |
| Molecular Weight | 608.63 |
| Formula | C28H31F3N4O6S |
| Cas No. | 2227149-22-4 |
| Smiles | C[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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 245 mg/mL (402.54 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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