2227149-22-4
2227149-22-4 structure
- Name: DS18561882
- Chemical Name: DS18561882
- CAS Number: 2227149-22-4
- Molecular Formula: C28H31F3N4O6S
- Molecular Weight: 608.63
- Catalog: Research Areas Cancer
- Create Date: 2019-12-08 13:51:19
- Modify Date: 2025-08-27 12:21:59
-
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile[1].
| Name | DS18561882 |
|---|
| Description | DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.0063 μM (MTHFD2); 0.57 μM (MTHFD1)[1] |
| In Vitro | DS18561882 (0-150 nM) gives the lowest GI50 value (140 nM) against the MDA-MB-231 cell line[1]. |
| In Vivo | DS18561882 (oral administration; 30, 100 or 300 mg/kg; twice daily) inhibits tumor growth inhibition with a dose-dependent manner, the tumor is completely inhibited (TGI: 67%) at the dose of 300 mg/kg in mice[1]. DS18561882 (oral administration; 10, 30, 100, or 300 mg/kg) has a good oral pharmacokinetic profile, including ACU (64.6, 264, 726 μg.h/ml ); Cmax (11.4, 56.5, 90.1 μg/ml); t1/2 (2.21, 2.16, 2.32 hours) for 30 mg/kg; 100mg/kg; 200 mg/kg, respectively[1]. DS18561882 is suspended in a 0.5% (w/v) methyl cellulose 400 solution in this article[1]. Animal Model: Five week old female BALB/cAJcl-nu/nu mice with MDA-MB-231 luc tumor cells (4 × 106 cells/mouse)[1] Dosage: 30, 100 or 300 mg/kg Administration: Oral administration; 30, 100 or 300 mg/kg; twice daily; until day 11 Result: Suppressed tumor growth in a dose-dependent manner. |
| References |
| Molecular Formula | C28H31F3N4O6S |
|---|---|
| Molecular Weight | 608.63 |