SML3497
LY345899
≥95% (HPLC)
Synonym(s):
5,6,7,8-Tetrahydro-N5,N10-carbonylfolic acid, LY 345899, LY-345899, LY354899, 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
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About This Item
Empirical Formula (Hill Notation):
C20H21N7O7
CAS Number:
Molecular Weight:
471.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
(Powder or Lyophilized powder or film)
Quality level:
Storage condition:
desiccated
Quality Level
assay
≥95% (HPLC)
form
(Powder or Lyophilized powder or film)
storage condition
desiccated
color
white to beige
storage temp.
-10 to -25°C
SMILES string
O=C1N2C3=C(NC(N)=NC3=O)NCC2CN1C4=CC=C(C=C4)C(N[C@H](C(O)=O)CCC(O)=O)=O
Biochem/physiol Actions
LY345899 (LY354899) is a methylenetetrahydrofolate dehydrogenase inhibitor (MTHFD1 IC50 = 96 nM with 30 μM folitixorin and 400 μM NADP+; MTHFD2 IC50 = 663 nM with 5 μM folitixorin and 250 μM NAD+) that exerts antiproliferation activity against cancer cells by targeting the folate cycle. Co-administer LY345899 with the dihydrofolate reductase (DHFR) inhibitor methotrexate (MTX) overcomes AML MTX resistance (50 mg/kg) in mice in vivo (10 mg/kg q.o.d. i.p.).
Methylenetetrahydrofolate dehydrogenase 1/2 (MTHFD1/2) inhibitor that exerts anti-cancer efficacy in vitro and in vivo by targeting the folate cycle.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Xinxin Ren et al.
Cancer research, 82(1), 60-74 (2021-11-13)
Metabolic reprogramming by oncogenic signaling is a hallmark of cancer. Hyperactivation of Wnt/β-catenin signaling has been reported in hepatocellular carcinoma (HCC). However, the mechanisms inducing hyperactivation of Wnt/β-catenin signaling and strategies for targeting this pathway are incompletely understood. In this
Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor.
Cancer Research, 77, 937-948 (2017)
Nadilly Bonagas et al.
Nature cancer, 3(2), 156-172 (2022-03-02)
The folate metabolism enzyme MTHFD2 (methylenetetrahydrofolate dehydrogenase/cyclohydrolase) is consistently overexpressed in cancer but its roles are not fully characterized, and current candidate inhibitors have limited potency for clinical development. In the present study, we demonstrate a role for MTHFD2 in