CB-5083 - 10mM in DMSO , CAS No.1542705-92-9

CAS: 1542705-92-9 Cat. No.: C408056 Fórmula: C₂₄H₂₃N₅O₂ Peso molecular: 413.47

CALIDAD & PUREZA 10mM in DMSO

Synonyms

1H-​Indole-​4-​carboxamide, 1-​[7,​8-​dihydro-​4-​[(phenylmethyl)​amino]​-​5H-​pyrano[4,​3-​d]​pyrimidin-​2-​yl]​-​2-​methyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
In vitro

In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM.

In vivo

In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition.
Cell Data

cell lines：

Concentrations：~40.0 μM

Incubation Time：72 h

Powder Purity:≥98%

Especificaciones

Sinónimos

1H-​Indole-​4-​carboxamide, 1-​[7,​8-​dihydro-​4-​[(phenylmethyl)​amino]​-​5H-​pyrano[4,​3-​d]​pyrimidin-​2-​yl]​-​2-​methyl-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.

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.

Tipo de acción

INHIBITOR

Propiedades del producto

ALogP

3.748

hba_count

4

Recuento HBD

2

Enlace rotable

5

Nombres e identificadores

Isómeros SMILES

CC1=CC2=C(C=CC=C2N1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5)C(=O)N

Peso molecular

413.47

Reaxy-Rn

26539278

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln=

Objetivos asociados (humanos)

VCP Tchem Transitional endoplasmic reticulum ATPase (6 Activities)

Discover Target: VCP

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• DMSO (mg/ml) Solubilidad máxima: 82
• DMSO (mM) Solubilidad máxima: 198.3215227
• Agua (mg/ml) Solubilidad máxima: ＜1