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DS18561882 

Cat. No.: HY-130251
Handling Instructions

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.

For research use only. We do not sell to patients.

DS18561882 Chemical Structure

DS18561882 Chemical Structure

CAS No. : 2227149-22-4

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10 mM * 1 mL in DMSO USD 496 Ask For Quote & Lead Time
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10 mg USD 550 Ask For Quote & Lead Time
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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].

IC50 & 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.
Molecular Weight

608.63

Formula

C₂₈H₃₁F₃N₄O₆S

CAS No.

2227149-22-4

SMILES

CS(=O)(NC1=CC=C(C(N2CCC(C3=CC=C(N4C[[email protected]](C)N(C)CC4)C(C)=C3O5)=C(C5=O)C2)=O)C=C1OC(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

DS18561882DS 18561882DS-18561882OthersInhibitorinhibitorinhibit

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