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TH9619 is an effective inhibitor of both dehydrogenase and cyclohydrolase activities in MTHFD1 and MTHFD2 (IC50=47 nM). It induces folate trapping and cell cycle arrest, thereby selectively killing cancer cells expressing MTHFD2.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $139 | - | In Stock | |
| 5 mg | $348 | - | In Stock | |
| 10 mg | $562 | - | In Stock | |
| 25 mg | $1,120 | - | In Stock | |
| 50 mg | $1,780 | - | In Stock | |
| 100 mg | $2,380 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $386 | - | In Stock |
| Description | TH9619 is an effective inhibitor of both dehydrogenase and cyclohydrolase activities in MTHFD1 and MTHFD2 (IC50=47 nM). It induces folate trapping and cell cycle arrest, thereby selectively killing cancer cells expressing MTHFD2. |
| 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 [1]. TH9619 (1 nM-1 μM, 96 hours) potently inhibits the proliferation of AML cells and T-ALL Jurkat cells [1]. TH9619 (1-100 μM, 96 hours) targets MTHFD1 (DC) in SW620 cells but demonstrates no significant targeting effect on mitochondrial MTHFD2 [2]. |
| 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 [1]. |
| Synonyms | TH-9619, TH 9619 |
| Molecular Weight | 451.37 |
| Formula | C17H18FN7O7 |
| Cas No. | 2379556-22-4 |
| 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 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (177.24 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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