SI-2
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- CAS-Nr.
- 380537-35-9
- Englisch Name:
- SI-2
- Synonyma:
- SI-2;(E)-SI-2;(E)SI2,(E) SI 2;1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-;Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
- CBNumber:
- CB33152741
- Summenformel:
- C15H15N5
- Molgewicht:
- 265.313
- MOL-Datei:
- 380537-35-9.mol
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SI-2 Eigenschaften
- Siedepunkt:
- 459.9±37.0 °C(Predicted)
- Dichte
- 1.22±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- Soluble in DMSO (up to 20 mg/ml).
- pka
- 11.05±0.70(Predicted)
- Aggregatzustand
- solid
- Farbe
- Pale orange
- Stabilit?t:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
SI-2 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
SI-2 is an inhibitor of steroid receptor coactivator-3 (SRC-3). Induces cell death in verious breast cancer cells.
Biochem/physiol Actions
SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC50?= 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice?in vivowith good pharmacokinetics (Cmax?= 30 μM,?tmax?= 0.25 h,?t1/2?= 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.
SI-2 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
SI-2 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 26)Lieferanten
380537-35-9()Verwandte Suche:
- SI-2
- Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
- 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
- (E)-SI-2
- (E)SI2,(E) SI 2
- 380537-35-9
