5.31000
Brk Inhibitor, Cpd 4f
Synonym(s):
Brk Inhibitor, Cpd 4f, PTK6 Inhibitor, Breast Tumor Kinase Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C17H13N3O
Molecular Weight:
275.30
NACRES:
NA.77
UNSPSC Code:
12352200
assay
≥97% (HPLC)
Quality Segment
form
powder
potency
3.15 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 100 mg/mL
storage temp.
−20°C
General description
A cell permeable pyridoindole based compound that acts as a highly potent and selective inhibitor of breast tumor kinase (Brk; IC50 = 3.15 nM) with minimal or no effect against a panel of more than 30 other protein kinases (IC50 = <10 µM for PIM2, NEK1 and2, CAMK4, MAPKAPK3 and 5 and MARK1, 3, and 5). Does not affect the activity of Akt isoforms, AGC kinases, ERK1 and 2, JNK 1 and 2 and HIPK isoforms. Displays anti-proliferative activity against multiple breast cancer cell lines (GI50 = 990 nM; 1.02 µM, and 1.58 µM for MCF7, HS-578/T, BT-549, respectively).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Brk
Brk
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are good for up to 2 weeks at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Mahmoud, K. A., et al. 2014. Bioorg. Med. Chem. Lett.24, 1948.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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