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Merck

SML3497

LY345899

≥95% (HPLC)

Synonym(e):

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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Über diesen Artikel

Empirische Formel (Hill-System):
C20H21N7O7
CAS-Nummer:
Molekulargewicht:
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

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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

assay

≥95% (HPLC)

form

(Powder or Lyophilized powder or film)

storage condition

desiccated

color

white to beige

storage temp.

-10 to -25°C

Quality Level

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Dieser Artikel
SML3411SML3637SML1438
form

(Powder or Lyophilized powder or film)

form

powder

form

(Powder or Lyophilized powder or film)

form

powder

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

-10 to -25°C

storage temp.

-10 to -25°C

storage temp.

-10 to -25°C

storage temp.

−20°C

storage condition

desiccated

storage condition

-

storage condition

-

storage condition

-

color

white to beige

color

white to beige

color

white to off-white

color

yellow to orange

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.

Lagerklasse

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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In der Dokumentenbibliothek finden Sie die Dokumentation zu den Produkten, die Sie kürzlich erworben haben.

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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
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
J L Tonkinson et al.
The Journal of pharmacology and experimental therapeutics, 287(1), 315-321 (1998-10-09)
5,6,7,8-Tetrahydro-N5,N10-carbonylfolic acid (LY354899) has been demonstrated to inhibit the dehydrogenase activity of C1-tetrahydrofolate synthase. This compound was only moderately antiproliferative toward CCRF-CEM lymphocytic leukemia cells in culture, but induced apoptosis after long incubation times. Slightly greater potency was observed in
Josep Tarragó-Celada et al.
Cancers, 13(3) (2021-01-28)
With most cancer-related deaths resulting from metastasis, the development of new therapeutic approaches against metastatic colorectal cancer (mCRC) is essential to increasing patient survival. The metabolic adaptations that support mCRC remain undefined and their elucidation is crucial to identify potential

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