Tyrphostin 9

製品コードS2895 バッチS289501

印刷

化学情報

Synonyms

SF 6847, RG-50872

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₂₂N₂O

分子量

282.38

CAS No.

10537-47-0

Solubility (25°C)*

体外

DMSO

56 mg/mL (198.31 mM)

Ethanol

56 mg/mL (198.31 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Tyrphostin 9（SF 6847、RG-50872）は、当初EGFR阻害剤としてIC50 460 μMで設計されましたが、PDGFRに対してはIC50 0.5 μMでより強力であることが判明しています。
in vitro	SF 6847 inhibits the replication of herpes simplex virus type 1 (HSV-1) with IC50 of 40 nM. SF 6847 (50 nM) partly reverses sodium orthovanadate induced HSV-1 plaque formation. SF 6847 (< 400 nM) decreases the phosphorylation of viral phosphoproteins in a dose-dependent manner, but the SF 6847 (< 800 nM)-induced reduction of protein synthesis is not dose-dependent. SF 6847 prevents PDGF-induced tyrosine phosphorylation of LRP in caveolae in human fibroblasts suggesting that PDGF-BB-mediated LRP activation requires tyrosine phosphorylation and therefore activation of PDGFR-β. SF 6847 (1 mM) blocks the strain-induced stimulatory effect on DNA synthesis of fetal lung cells. SF 6847 (1 μM) causes increased exon inclusion of MAPT exon 10. SF 6847 does not affect the translation or stability of the two mRNAs. SF 6847 (1.6 μM) increases the inclusion of MAPT exon 10 by 2-fold in SHSY-5Y cells.

製品説明

Tyrphostin 9（SF 6847、RG-50872）は、当初EGFR阻害剤としてIC50 460 μMで設計されましたが、PDGFRに対してはIC50 0.5 μMでより強力であることが判明しています。

in vitro

SF 6847 inhibits the replication of herpes simplex virus type 1 (HSV-1) with IC50 of 40 nM. SF 6847 (50 nM) partly reverses sodium orthovanadate induced HSV-1 plaque formation. SF 6847 (< 400 nM) decreases the phosphorylation of viral phosphoproteins in a dose-dependent manner, but the SF 6847 (< 800 nM)-induced reduction of protein synthesis is not dose-dependent. SF 6847 prevents PDGF-induced tyrosine phosphorylation of LRP in caveolae in human fibroblasts suggesting that PDGF-BB-mediated LRP activation requires tyrosine phosphorylation and therefore activation of PDGFR-β. SF 6847 (1 mM) blocks the strain-induced stimulatory effect on DNA synthesis of fetal lung cells. SF 6847 (1 μM) causes increased exon inclusion of MAPT exon 10. SF 6847 does not affect the translation or stability of the two mRNAs. SF 6847 (1.6 μM) increases the inclusion of MAPT exon 10 by 2-fold in SHSY-5Y cells.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	The cells are solubilized in 1 mL per 2×10⁷ cells of cold solubilization buffer (50 mM Hepes buffer, pH 7.6, 1% Triton X-100, 150 mM NaCl, 5 mM EGTA, 1 mM PMSF, 50 pg/mL aprotinin, 25 mM benzamidine, 5 pg/mL leupeptin, and 10 kg/mL soybean trypsin inhibitor) for 20 min at 4 ℃. After centrifugation at 1×10⁷g for 30 min, the supernatant is loaded onto a WGA-agarose column and shaken for 2 hours at 4 ℃. The unabsorbed material is removed and the resin is washed twice with HTN buffer (50 mM Hepes, pH 7.6, 0.1% Triton X-100, 150 mM NaCl), twice with HTN buffer containing 1 M NaCl, and twice with HTNG buffer (50 mM Hepes, pH 7.6, 0.1% Triton X-100, 150 mM NaCl, and 10% glycerol). The EGF receptor is eluted batchwise with HTNG buffer containing 0.5 M NADG. The eluted material is stored in aliquots at -70℃ and diluted before use with TMTNG buffer (50 mM Tris-Mes buffer, pH 7.6, 0.1% Triton X-100, 150 mM NaCl, 10% glycerol).

参考

https://pubmed.ncbi.nlm.nih.gov/2552117/
https://pubmed.ncbi.nlm.nih.gov/7544112/
https://pubmed.ncbi.nlm.nih.gov/11854295/

https://pubmed.ncbi.nlm.nih.gov/7653578/
https://pubmed.ncbi.nlm.nih.gov/18678901/
https://pubmed.ncbi.nlm.nih.gov/2143901/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Mutant CHCHD10 causes an extensive metabolic rewiring that precedes OXPHOS dysfunction in a murine model of mitochondrial cardiomyopathy [ Cell Rep, 2022, 38(10):110475]	PubMed: 35263592

Mutant CHCHD10 causes an extensive metabolic rewiring that precedes OXPHOS dysfunction in a murine model of mitochondrial cardiomyopathy [ Cell Rep, 2022, 38(10):110475]

PubMed: 35263592

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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