GRADE & PURITY 10mM in DMSO

Synonyms

L-​Norleucine,6-​diazo-​N-​[[(2,​2-​dimethyl-​1-​oxopropoxy)​phenylmethoxy]​carbonyl]​-​5-​oxo-​,1-​methylethyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.

Targets

Glutamine

In vitro

JHU395 inhibits growth of multiple biosynthetic processes by tumors (MPNST) cells, while growth of immortalized Schwann cells is minimally affected. JHU395 induces less PARP cleavage as a marker of apoptosis in human MPNST cells. JHU395 is a plasma stable lipophilic GA prodrug which delivers DON to MPNST in an in vitro plasma to tumor cell partitioning assay measurement.

In vivo

orally administered JHU395 delivers active GA to tumors with over twofold higher tumor-to-plasma exposure, and significantly inhibits tumor growth in a murine flank MPNST model without observed toxicity.

Cell Research(from reference)

Cell lines：sNF96.2, sNF02.2, ipn02.32 

Concentrations：10 μM, 20μM 

Incubation Time：1 h, 24 h 

Specifications

Sinónimos

L-​Norleucine, 6-​diazo-​N-​[[(2, ​2-​dimethyl-​1-​oxopropoxy)​phenylmethoxy]​carbonyl]​-​5-​oxo-​, 1-​methylethyl ester

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and sig

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Propiedades del producto

• ALogP: 4.148
• Recuento HBD: 1
• Enlace rotable: 14

Nombres e identificadores

• Sonrisas canónicas: CC(C)OC(=O)C(CCC(=O)C=[N+]=N)NC(=O)OC(C1=CC=CC=C1)OC(=O)C(C)(C)C
• IUPAC Name: [(5S)-5-[[2,2-dimethylpropanoyloxy(phenyl)methoxy]carbonylamino]-2,6-dioxo-6-propan-2-yloxyhexylidene]-iminoazanium
• InChIKey: KCTDLEPDMHFLHZ-KKFHFHRHSA-O
• INCHI: 1S/C22H29N3O7/c1-14(2)30-18(27)17(12-11-16(26)13-24-23)25-21(29)32-19(15-9-7-6-8-10-15)31-20(28)22(3,4)5/h6-10,13-14,17,19,23H,11-12H2,1-5H3/p+1/t17-,19?/m0/s1
• PubChem CID: 126555751
• Peso molecular: 447.48