An ATP-competitive Raf kinase inhibitor (IC50s = 0.64

Dabrafenib – 5 mg

Brand:
Cayman
CAS:
1195765-45-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Dabrafenib is an ATP-competitive inhibitor of Raf kinases (IC50s = 0.64, 0.68, and 5 nM for wild-type B-RAF kinase, mutant B-RAFV600E, and wild-type C-RAF kinase, respectively).{42963} It also inhibits the tyrosine kinase-like kinases ALK5 and LIMK1 (IC50s = 11 and 15 nM, respectively) and the calcium/calmodulin-dependent protein kinases SIK2 and PDK2 (IC50s = 27 and 57 nM, respectively), as well as NEK11, CK1, and BRK (IC50s = 20, 41, and 79 nM, respectively) in a panel of 270 kinases at 300 nM. Dabrafenib inhibits the growth of 16 cancer cell lines expressing mutant B-RAFV600E (GI50s = 50s = 50s = V600E, 133 cell lines expressing wild-type Ras and Raf, or 18 cell lines expressing mutant Ras (GI50s = >10 µM) in a panel of 195 cancer cell lines. Dabrafenib (8 nM) inhibits MAPK signaling, inhibiting phosphorylation of MEK and ERK, and activates caspase-3/7 in B-RAFV600E-expressing A375P melanoma cells but not in wild-type B-RAF-expressing human foreskin fibroblasts (EC200s =71 and >10,000 nM, respectively). It reduces tumor growth in an A375P mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg. Formulations containing dabrafenib have been used in the treatment of B-RAFV600E-expressing cancers.  

 

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Description

An ATP-competitive Raf kinase inhibitor (IC50s = 0.64, 0.68, and 5 nM for wild-type B-RAF kinase, mutant B-RAFV600E, and wild-type C-RAF kinase, respectively); also inhibits ALK5, LIMK1, SIK2, PDK2, NEK11, CK1, and BRK (IC50s = 11, 15, 27, 57, 20, 41, and 79 nM, respectively) in a panel of 270 kinases at 300 nM; inhibits the growth of 16 cancer cell lines expressing mutant B-RAFV600E (GI50s = 50s = 50s = V600E-expressing A375P melanoma cells; reduces tumor growth in an A375P mouse xenograft model at 3-100 mg/kg

Formal name: N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide

Synonyms:  GSK2118436

Molecular weight: 519.6

CAS: 1195765-45-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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