121767
AG 1024
A cell-permeable, reversible, substrate competitive, and specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity.
Synonym(s):
AG 1024, 3-Bromo-5- t-butyl-4-hydroxy-benzylidenemalonitrile
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About This Item
Empirical Formula (Hill Notation):
C14H13BrN2O
CAS Number:
Molecular Weight:
305.17
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white to yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Brc1c(c(cc(c1)C=C(C#N)C#N)C(C)(C)C)O
InChI
1S/C14H13BrN2O/c1-14(2,3)11-5-9(4-10(7-16)8-17)6-12(15)13(11)18/h4-6,18H,1-3H3
InChI key
ABBADGFSRBWENF-UHFFFAOYSA-N
General description
A cell-permeable, reversible, substrate competitive, and specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor kinases with significantly lower IC50 values for IGF-1 than for insulin receptors. Induces apoptosis by downregulating the expression of phospho-Akt1 and Bcl-2; and increasing the expression of Bax, p53 and p21. Reported to enhance the radiosensitivity of human breast cancer cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IGF-1
IGF-1
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 2 months at -20°C.
Other Notes
Wen, B., et al. 2001. Br. J. Cancer85, 2017.
Parrizas, M., et al. 1997. Endocrinology138, 1427.
Ohmichi, M., et al. 1993. Biochemistry32, 4650.
Parrizas, M., et al. 1997. Endocrinology138, 1427.
Ohmichi, M., et al. 1993. Biochemistry32, 4650.
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
Certificates of Analysis (COA)
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