An MTHFD inhibitor
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LY345899

Item No. 36627

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(3-amino-1,2,5,6,6a,7-hexahydro-1,9-dioxoimidazo[1,5-f]pteridin-8(9H)-yl)benzoyl]-L-glutamic acid
CAS Number
10538-99-5
Molecular Formula
C20H21N7O7
Formula Weight
471.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
293 nm
SMILES
O=C1N2C3=C(NC(N)=NC3=O)NCC2CN1C4=CC=C(C=C4)C(N[C@H](C(O)=O)CCC(O)=O)=O
InChi Code
InChI=1S/C20H21N7O7/c21-19-24-15-14(17(31)25-19)27-11(7-22-15)8-26(20(27)34)10-3-1-9(2-4-10)16(30)23-12(18(32)33)5-6-13(28)29/h1-4,11-12H,5-8H2,(H,23,30)(H,28,29)(H,32,33)(H4,21,22,24,25,31)/t11?,12-/m0/s1
InChi Key
JSNFRYBHBVDHSG-KIYNQFGBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $304

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    25 mg

    $542

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    Cayman Chemical
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    Product Description

    LY345899 is an inhibitor of methylenetetrahydrofolate dehydrogenase 1 (MTHFD1) and MTHFD2 (IC50s = 96 and 663 nM, respectively).1 It decreases the NADPH-to-NADP+ (NADPH/NADP+) and reduced glutathione-to-oxidized glutathione (GSH/GSSG) ratios and increases the production of reactive oxygen species (ROS) in HCT116, SW620, and LoVo colorectal cancer cells when used at a concentration of 10 µM.2 LY345899 is cytotoxic to SW620 and LoVo cells, an effect that can be reversed by the antioxidant N-acetyl-L-cysteine (NAC; Item No. 20261). In vivo, LY345899 (10 mg/kg) reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gustafsson, R., Jemth, A.-S., Gustafsson, N.M.S., et al. Crystal structure of the emerging cancer target MTHFD2 in complex with a substrate-based inhibitor. Cancer Res. 77(4), 937-948 (2017).

    2. Ju, H.-Q., Lu, Y.-X., Chen, D.-L., et al. Modulation of redox homeostasis by inhibition of MTHFD2 in colorectal cancer: Mechanisms and therapeutic implications. J. Natl. Cancer Inst. 111(6), 584-596 (2109).