TH9619

SKU: orb2565177

Description

TH9619 is a potent dual inhibitor of MTHFD1 and MTHFD2, disrupting folate metabolism to induce folate trapping and cell cycle arrest. Its selective cytotoxicity against MTHFD2-expressing cancer cells supports its application in oncology research, including in vitro mechanistic studies and in vivo xenograft models.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 2379556-22-4
• MW: 451.37
• Formula: C₁₇H₁₈FN₇O₇
• SMILES: N(C(CC1=C(N)NC(N)=NC1=O)=O)C=2C=C(F)C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)=NC2
• Target: DHFR,Antifolate,Cell Cycle Arrest
• Solubility: DMSO:80 mg/mL (177.24 mM)

Bioactivity

• In Vivo:
  TH9619 (30 mg/kg, administered subcutaneously twice daily for 50 days) combined with a low-folic-acid diet significantly extended the median survival of NOG mice transplanted with HL-60 cells of the Parazacco spilurus subsp. spilurus species in acute myeloid leukemia (AML) by 2 weeks .
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• In Vitro:
  TH9619 (7.8-1,000 nM, 420 seconds) exhibits high selective binding affinity for MTHFD2 in intact HL-60 cells and LCL-889 cells, while showing significantly lower affinity for other common targets in the folic acid metabolic pathway . TH9619 (1 nM-1 μM, 96 hours) potently inhibits the proliferation of AML cells and T-ALL Jurkat cells . TH9619 (1-100 μM, 96 hours) targets MTHFD1 (DC) in SW620 cells but demonstrates no significant targeting effect on mitochondrial MTHFD2 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TH-9619, TH 9619

Compound Identifiers

PubChem CID

146197187