An MTHFD inhibitor
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TH9619

Item No. 45380

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[5-[[2-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)acetyl]amino]-3-fluoro-2-pyridinyl]carbonyl]-L-glutamic acid
CAS Number
2379556-22-4
Molecular Formula
C17H18FN7O7
Formula Weight
451.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
NC(NC(N)=NC1=O)=C1CC(NC2=CN=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C(F)=C2)=O
InChi Code
InChI=1S/C17H18FN7O7/c18-8-3-6(22-10(26)4-7-13(19)24-17(20)25-14(7)29)5-21-12(8)15(30)23-9(16(31)32)1-2-11(27)28/h3,5,9H,1-2,4H2,(H,22,26)(H,23,30)(H,27,28)(H,31,32)(H5,19,20,24,25,29)/t9-/m0/s1
InChi Key
ALGPVOJFIGPPPX-VIFPVBQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $95

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    5 mg

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    10 mg

    $665

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    Cayman Chemical
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    Product Description

    TH9619 is an inhibitor of methylenetetrahydrofolate dehydrogenase 1 (MTHFD1), MTHFD2, and MTHFD2L (IC50s = 16, 47, and 47 nM, respectively), enzymes often overexpressed in cancer.1 It inhibits nuclear MTHFD2 and cytoplasmic MTHFD1 but not mitochondrial MTHFD2, leading to an increase in 10-formyl-tetrahydrofolate (10-CHO-THF), thymidylate depletion, and cell death.2 It is selective for MTHFD1 and MTHFD2 over a panel of 44 kinases at 12 µM and reduces proliferation in a panel of acute myeloid leukemia (AML) cells, including HL-60 and THP-1 cells, in a concentration-dependent manner. TH9619 (50 nM) impairs DNA replication in HL-60 and THP-1 cells but not non-tumorigenic LCL-534 and LCL-889 lymphocytes. It increases survival in an HL-60 mouse xenograft model when administered at a dose of 30 mg/kg twice per day in combination with a low-folate diet.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bonagas, N., Gustafsson, N.M.S., Henriksson, M., et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nat. Cancer 3(2), 156-172 (2022).

    2. Green, A.C., Marttila, P., Kiweler, N., et al. Formate overflow drives toxic folate trapping in MTHFD1 inhibited cancer cells. Nat. Metab. 5(4), 642-659 (2023).