ChemicalBook--->CAS DataBase List--->149286-90-8

149286-90-8

149286-90-8 Structure

149286-90-8 Structure
IdentificationBack Directory
[Name]

RG-13022
[CAS]

149286-90-8
[Synonyms]

[Molecular Formula]

C16H14N2O2
[MDL Number]

MFCD00906755
[MOL File]

149286-90-8.mol
[Molecular Weight]

266.295
Chemical PropertiesBack Directory
[Boiling point ]

423.8±45.0 °C(Predicted)
[density ]

1.172±0.06 g/cm3(Predicted)
[solubility ]

DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml; Ethanol: 2 mg/ml
[form ]

A crystalline solid
[pka]

3.74±0.12(Predicted)
Hazard InformationBack Directory
[Description]

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 μM in HT-22 cells.
[Uses]

(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells[1][2].
[Definition]

ChEBI: 3-(3,4-dimethoxyphenyl)-2-(3-pyridinyl)-2-propenenitrile is a dimethoxybenzene.
[References]

[1] Reddy KB, et al. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res. 1992 Jul 1;52(13):3636-41. PMID:1617636
[2] McLeod HL, et al. In vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor RG13022. Br J Cancer. 1996 Dec;74(11):1714-8. DOI:10.1038/bjc.1996.620
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