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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 |
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 |
Storage | ||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (131.44 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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