An inhibitor of Raf kinases (Kis = 0.3

B-RAF Inhibitor 1 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1191385-19-9
Storage:
-20
UN-No:
Non-Hazardous - /

B-RAF inhibitor 1 is an inhibitor of Raf kinases (Kis = 0.3, 1, and 1 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45545} It is selective for the B-RAFV600E kinase domain over Lck, Tie2, KDR, and p38α (IC50s = 83, 120, 1,000, and >1,600 nM, respectively).{45546} B-RAF inhibitor 1 inhibits phosphorylation of ERK in A375 melanoma cells (IC50 = 1.8 nM). It reduces tumor growth in an A375 SQ2 mouse xenograft model (ED50 = 1.3 mg/kg per day) and induces 85% tumor regression when administered at a dose of 5 mg/kg per day for 14 days. B-RAF inhibitor 1 (5 and 10 mg/kg per day) increases tumor growth in a MIA PaCa-2 mouse xenograft model.{45545}  

 

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SKU: 26792 - 5 mg Category:

Description

An inhibitor of Raf kinases (Kis = 0.3, 1, and 1 nM for C-RAF, B-RAF, and B-RAFV600E, respectively); selective for B-RAFV600E kinase domain over Lck, Tie2, KDR, and p38α (IC50s = 83, 120, 1,000, and >1,600 nM, respectively); inhibits phosphorylation of ERK in A375 melanoma cells (IC50 = 1.8 nM); reduces tumor growth in an A375 SQ2 mouse xenograft model (ED50 = 1.3 mg/kg per day) and induces 85% tumor regression at 5 mg/kg per day for 14 days; increases tumor growth in a MIA PaCa-2 mouse xenograft model at 5 and 10 mg/kg per day

Formal name: N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine, dihydrochloride

Synonyms: 

Molecular weight: 551.9

CAS: 1191385-19-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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