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 Molecular Weight: 519.56 EC Number: 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

Overview

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

Synonyms

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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

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

Names and Identifiers

• Isomeric 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
• Molecular Weight: 519.56
• Reaxy-Rn: 19689971
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19689971&ln=

Associated Targets(Human)

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)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 71 mg/mL (198.1 mM)
• Refractive Index: 1.63
• Boil Point(°C): ~653.7 °C at 760 mmHg

References

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]