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Key Documents

SML3497

Sigma-Aldrich

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
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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