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Merck
CN

5.31000

Brk Inhibitor, Cpd 4f

别名:

Brk Inhibitor, Cpd 4f, PTK6 Inhibitor, Breast Tumor Kinase Inhibitor

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关于此项目

经验公式(希尔记法):
C17H13N3O
分子量:
275.30
NACRES:
NA.77
UNSPSC Code:
12352200
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assay

≥97% (HPLC)

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

Quality Level

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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