An MTHFD inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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 (Request formulation change)
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $44

    Add

    5 mg

    $174

    Add

    10 mg

    $304

    Add

    25 mg

    $542

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    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).