Saltar al contenido
MilliporeSigma
Todas las fotos(1)

Documentos clave

Ver Toda la documentación

SML2772

Sigma-Aldrich

SAR405838

≥98% (HPLC)

Sinónimos:

(2′S,3R,4′S,5′R)-6-Chloro-4′-(3-chloro-2-fluorophenyl)-2′-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxospiro[3H-indole-3,3′-pyrrolidine]-5′-carboxamide, MI 77301, MI-77301, MI77301

Iniciar sesiónpara Ver la Fijación de precios por contrato y de la organización

Seleccione un Tamaño

1 MG
$68.78
5 MG
$268.00

$68.78

Precio de catálogo$72.40Ahorre 5 %

En stockDetalles

Todas las fotos(1)

Seleccione un Tamaño

Cambiar Vistas
1 MG
$68.78
5 MG
$268.00

About This Item

Fórmula empírica (notación de Hill):
C29H34Cl2FN3O3
Número de CAS:
1303607-60-4
Peso molecular:
562.50
Número MDL:
MFCD28976052
Código UNSPSC:
12352200
NACRES:
NA.77

$68.78

Precio de catálogo$72.40Ahorre 5 %

En stockDetalles

Nivel de calidad

100

Ensayo

≥98% (HPLC)

condiciones de almacenamiento

desiccated

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

cadena SMILES

O=C([C@@H]1N[C@@H](CC(C)(C)C)[C@@]2(C(NC3=C2C=CC(Cl)=C3)=O)[C@H]1C4=CC=CC(Cl)=C4F)N[C@@H]5CC[C@H](CC5)O

InChI

1S/C29H34Cl2FN3O3/c1-28(2,3)14-22-29(19-12-7-15(30)13-21(19)34-27(29)38)23(18-5-4-6-20(31)24(18)32)25(35-22)26(37)33-16-8-10-17(36)11-9-16/h4-7,12-13,16-17,22-23,25,35-36H,8-11,14H2,1-3H3,(H,33,37)(H,34,38)/t16-,17-,22-,23-,25+,29+/m0/s1

Clave InChI

IDKAKZRYYDCJDU-HBMMIIHUSA-N

Acciones bioquímicas o fisiológicas

Orally available, highly potent and selective Mdm2 (Hdm2) inhibitor that blocks cancer growth in a wild-type p53-dependent manner both in vitro and in vivo.
SAR405838 (MI-77301) is an orally available (F = 67%/mouse, 48%/rat; 10 mg/kg p.o.), highly potent and selective Mdm2 (Hdm2) inhibitor (human Mdm2 Ki = 0.88 nM; no binding at 10 μM to Bcl-2, Bcl-xL, Mcl-1, Mdmx; no inhibition against >200 receptors/enzymes) that upregulates wild-type p53 activity (EC50 = 300-600 nM; SJSA-1) by blocking Mdm2-p53 interaction and Mdm2-mediated p53 degradation with 5-10-times higher potency than MI-219 and nutlin-3a. SAR405838 inhibits cancer growth in a wild-type p53-dependent manner both in cultures (IC50 = 89 nM/RS4;11, 92 nM/SJSA-1, 200 nM/HCT-116, 270 nM/LANCaP) and in xenograft models in vivo (50-200 mg/kg single or daily p.o. dosing).

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Elija entre una de las versiones más recientes:

Certificados de análisis (COA)

Lot/Batch Number
0000418834
0000418834

¿No ve la versión correcta?

Si necesita una versión concreta, puede buscar un certificado específico por el número de lote.

Busque por un COA

¿Ya tiene este producto?

Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.

Visite la Librería de documentos

Liye He et al.
Cancer research, 78(9), 2407-2418 (2018-02-28)
The molecular pathways that drive cancer progression and treatment resistance are highly redundant and variable between individual patients with the same cancer type. To tackle this complex rewiring of pathway cross-talk, personalized combination treatments targeting multiple cancer growth and survival
A N Hata et al.
Oncogene, 36(47), 6581-6591 (2017-08-08)
There are currently no effective targeted therapies for KRAS mutant cancers. Therapeutic strategies that combine MEK inhibitors with agents that target apoptotic pathways may be a promising therapeutic approach. We investigated combining MEK and MDM2 inhibitors as a potential treatment
Maja de Jonge et al.
European journal of cancer (Oxford, England : 1990), 76, 144-151 (2017-03-23)
In tumours with wild-type TP53, the tumour-suppressive function of p53 is frequently inhibited by HDM2. This phase I, dose-escalating study investigated the maximum tolerated dose (MTD), safety, pharmacokinetics and pharmacodynamics of SAR405838, an HDM2 inhibitor, in patients with advanced solid tumours (NCT01636479).
Sana AlQarni et al.
Oncogene, 37(29), 3998-4012 (2018-04-25)
Epstein-Barr virus (EBV)-associated Burkitt's lymphoma is characterised by the deregulation of c-Myc expression and a restricted viral gene expression pattern in which the EBV nuclear antigen-1 (EBNA1) is the only viral protein to be consistently expressed. EBNA1 is required for
Kate Lynn J Bill et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 22(5), 1150-1160 (2015-10-18)
Dedifferentiated liposarcoma (DDLPS) is an aggressive malignancy that can recur locally or disseminate even after multidisciplinary care. Genetically amplified and expressed MDM2, often referred to as a "hallmark" of DDLPS, mostly sustains a wild-type p53 genotype, substantiating the MDM2:p53 axis
Ver todos los artículos relacionados

Questions

Reviews

No rating value

Active Filters

Nuestro equipo de científicos tiene experiencia en todas las áreas de investigación: Ciencias de la vida, Ciencia de los materiales, Síntesis química, Cromatografía, Analítica y muchas otras.

Póngase en contacto con el Servicio técnico