Dabrafenib (GSK2118436) - Moligand™, 10mM in DMSO , Inhibitor of B-Raf proto-oncogene; serine/threonine kinase, CAS No.1195765-45-7, Inhibitor of B-Raf proto-oncogene; serine/threonine kinase

CAS: 1195765-45-7 Cat. No.: D409111 Peso molecular: 519.56 Número EC: 689-166-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GSK2118436A | N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Dabrafenib (GSK2118436, GSK2118436A) is a mutantBRAFV600specific inhibitor withIC50of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
In vitro

Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-Raf^V600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-Raf^V600E.

In vivo

Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

GSK2118436A | N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2, 6-difluorobenzenesulfonamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

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.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of B-Raf proto-oncogene; serine/threonine kinase

Nombres e identificadores

• Isómeros SMILES: CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F
• Peso molecular: 519.56
• Reaxy-Rn: 19689971
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19689971&ln=

Objetivos asociados (humanos)

CDK16 Tchem Cyclin-dependent kinase 16 (1 Activities)

Discover Target: CDK16

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

CDK2 Tchem Cyclin-dependent kinase 2 (1 Activities)

Discover Target: CDK2

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

RIPK3 Tchem Receptor-interacting serine/threonine-protein kinase 3 (1 Activities)

Discover Target: RIPK3

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

BRAF Tclin Serine/threonine-protein kinase B-raf (21 Activities)

Discover Target: BRAF

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

ARAF Tchem Serine/threonine-protein kinase A-Raf (1 Activities)

Discover Target: ARAF

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

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 71 mg/mL (198.1 mM)
• Índice de refracción: 1.63
• Punto de ebullición (°C): ~653.7 °C at 760 mmHg

Referencias

1. Yunsheng Ran, Chujiao Hu, Junzhao Wan, Qian Kang, Ruixian Zhou, Ping Liu, Dan Ma, Jianta Wang, Lei Tang.  (2023)  Integrated investigation and experimental validation of PPARG as an oncogenic driver: implications for prognostic assessment and therapeutic targeting in hepatocellular carcinoma.  Frontiers in Pharmacology,      [PMID:38044948] [10.3389/fphar.2023.1298341]

2. Jinling Cui, Mingzhu Yan, Xiaoyi Liu, Shutao Yin, Shangyun Lu, Lihong Fan, Hongbo Hu.  (2019)  Inorganic Selenium Induces Nonapoptotic Programmed Cell Death in PC-3 Prostate Cancer Cells Associated with Inhibition of Glycolysis.  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:31513389] [10.1021/acs.jafc.9b03875]

3. Jie Liang, Dong-Kun Zhao, Hao-Ming Yin, Tai-Yu Tian, Jian-Kang Kang, Song Shen, Jun Wang.  (2025)  Combinatorial screening of nanomedicines in patient-derived cancer organoids facilitates efficient cancer therapy.  Nano Today,      [PMID:] [10.1016/j.nantod.2025.102665]

4. QIAN HU, MENGYAO WANG, JINJIN WANG, YALI TAO, TING NIU.  (2024)  Development of a cell adhesion-based prognostic model for multiple myeloma: Insights into chemotherapy response and potential reversal of adhesion effects.  ONCOLOGY RESEARCH,      [PMID:38560563] [10.32604/or.2023.043647]