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RG 13022

SKU: orb1223332

Description

RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 μM in HT-22 cells. Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs.

Images & Validation

Key Properties

CAS Number136831-48-6
MW266.29
Purity>98% (HPLC)
FormulaC16H14N2O2
SMILESCOc1c(cc(cc1)/C=C(\C#N)/c1cnccc1)OC
TargetEGFR
SolubilityIn Vitro: DMSO : 100 mg/mL (375.53 mM)

Bioactivity

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

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

RG 13022 | RG-13022.Tyrphostin RG 13022

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RG 13022 (orb1223332)

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200 mg
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2 mg
$ 80.00
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$ 100.00
10 mg
$ 140.00
25 mg
$ 270.00
50 mg
$ 440.00
100 mg
$ 680.00