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
• Empirical Formula (Hill Notation): C₁₄H₁₃BrN₂O
• CAS Number: 65678-07-1
• Molecular Weight: 305.17
• MDL number: MFCD02179365
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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.

A cell-permeable, reversible, substrate competitive, and specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC₅₀ values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
IGF-1

Product does not compete with ATP.

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3