Catalog No. Size 价格库存数量
S0861-2 2mg solid ¥100
售罄
不可用
S0861-10 10mg solid ¥300
售罄
不可用

详情描述

RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.

Product information

CAS Number: 136831-48-6

Molecular Weight: 266.29

Formula: C16H14N2O2

Synonym:

Tyrphostin RG13022

Chemical Name: (2E)-3-(3, 4-dimethoxyphenyl)-2-(pyridin-3-yl)prop-2-enenitrile

Smiles: COC1=CC(/C=C(/C#N)\C2=CN=CC=C2)=CC=C1OC

InChiKey: DBGZNJVTHYFQJI-ZSOIEALJSA-N

InChi: InChI=1S/C16H14N2O2/c1-19-15-6-5-12(9-16(15)20-2)8-14(10-17)13-4-3-7-18-11-13/h3-9,11H,1-2H3/b14-8-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

RG13022 suppresses EGF-stimulated cancer cell proliferation. In a cell-free reaction RG13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with an IC50 of 4 μM. RG13022 inhibits colony formation and DNA synthesis by HER 14 cells, which were stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50s are 1 and 3 μM for HER 14 colony formation and DNA synthesis, respectively. RG-13022 inhibits not only EGF-induced growth but also growth stimulated by insulin, insulin-like growth factor I, insulin-like growth factor II, or transforming growth factor alpha. RG-13022 also totally blocks estrogen-stimulated phosphorylation of the EGF receptor, as well as estrogen-induced cell proliferation, suggesting that functioning TK pathways are required for estrogen action.

In Vivo:

RG13022 suppresses tumor growth in nude mice. RG13022 also increases the life span of these tumor-bearing nude mice.

References:

  1. Yoneda T, et al. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5.
  2. 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.

Products are for research use only. Not for human use.

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