Saltar al contenido
Merck
Todas las fotos(1)

Documentos clave

Ver Toda la documentación

SML2154

Sigma-Aldrich

Deltarasin trihydrochloride

≥98% (HPLC)

Sinónimos:

(S)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole trihydrochloride, 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride

Iniciar sesiónpara Ver la Fijación de precios por contrato y de la organización
Todas las fotos(1)

About This Item

Fórmula empírica (notación de Hill):
C40H37N5O · 3HCl
Número de CAS:
1440898-61-2
Peso molecular:
713.14
Código UNSPSC:
12352200
NACRES:
NA.77

Ensayo

≥98% (HPLC)

Formulario

powder

condiciones de almacenamiento

desiccated

color

white to beige

solubilidad

H2O: 2 mg/mL, clear

temp. de almacenamiento

2-8°C

cadena SMILES

N1CCC(CC1)[C@H]([n]6c7c(nc6c8ccccc8)cccc7)COc2ccc(cc2)c3[n](c5c(n3)cccc5)Cc4ccccc4

InChI

1S/C40H37N5O/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31/h1-22,30,38,41H,23-28H2/t38-/m1/s1

Clave InChI

LTZKEDSUXKTTTC-KXQOOQHDSA-N

Acciones bioquímicas o fisiológicas

Deltarasin is a membrane-permeable benzimidazole derivative that effectively abolishes cellular KRas plasma membrane localization (5 μM for 1 hr) by blocking KRas-PDEδ interaction via high affinity interaction with PDEδ prenyl-binding pocket (KD = 38 nM). Deltarasin inhibits oncogenic KRas-dependent proliferation (by ~50% of Panc-Tu-I cells; 5μM for 70 hrs) and survival (52% and 46% death induction of Panc-Tu-I and Capan-1 cells, respectively; 5μM for 24 hrs) in human pancreatic ductal adenocarcinoma (PDAC) cultures and is efficacious against Panc-Tu-I xenograft-derived tumor growth in mice in vivo (60% and 80% retardation on day 9, respectively, with 15 mg/kg q.d. or 10 mg/kg b.i.d. via i.p.).
KRas-PDEδ interaction blocker that targets PDEδ prenyl pocket with high affinity and inhibits oncogenic KRas-dependent cancer survival in vitro and in vivo.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Elija entre una de las versiones más recientes:

Certificados de análisis (COA)

Lot/Batch Number
0000230817
0000227258

¿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

Pablo Martín-Gago et al.
Angewandte Chemie (International ed. in English), 56(9), 2423-2428 (2017-01-21)
Small-molecule inhibition of the interaction between the KRas oncoprotein and the chaperone PDE6δ impairs KRas spatial organization and signaling in cells. However, despite potent binding in vitro (K
Philipp Küchler et al.
Bioorganic & medicinal chemistry, 26(8), 1426-1434 (2017-09-25)
Prenylation is a post-translational modification that increases the affinity of proteins for membranes and mediates protein-protein interactions. The retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta (PDEδ) is a prenyl binding protein that is essential for the shuttling of small
Jianman Guo et al.
American journal of cancer research, 7(4), 923-934 (2017-05-05)
Patients with Neurofibromatosis type 1 (NF1) and Neurofibromatosis type 2 (NF2) are predisposed to tumors of the nervous system. NF1 patients predominantly develop neurofibromas, and Malignant Peripheral Nerve Sheath Tumors (MPNST) while NF2 patients develop schwannomas and meningiomas. Here we
Gunther Zimmermann et al.
Journal of medicinal chemistry, 57(12), 5435-5448 (2014-06-03)
K-Ras is one of the most frequently mutated signal transducing human oncogenes. Ras signaling activity requires correct cellular localization of the GTPase. The spatial organization of K-Ras is controlled by the prenyl binding protein PDEδ, which enhances Ras diffusion in
Gunther Zimmermann et al.
Nature, 497(7451), 638-642 (2013-05-24)
The KRAS oncogene product is considered a major target in anticancer drug discovery. However, direct interference with KRAS signalling has not yet led to clinically useful drugs. Correct localization and signalling by farnesylated KRAS is regulated by the prenyl-binding protein
Ver todos los artículos relacionados

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