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Moligand™, 10mM in DMSO Moligand™ für empfindliche chromatographische und analytische Workflows, die minimale Basislinieninterferenzen erfordern.
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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
SNS-032 (BMS-387032) has firstly been described as a selective inhibitor ofCDK2withIC50of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive toCDK7/9withIC50of 62 nM/4 nM, with little effect on CDK6
In vitro
SNS-032 has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. SNS-032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS-032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS-032 activity is readily reversible; removal of SNS-032 reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival. SNS-032 inhibits three dimensional capillary network formations of endothelial cells. SNS-032 completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, SNS-032 significantly prevents the production of VEGF in both cell lines, SNS-032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS-032 induces cell cycle arrest and apoptosis across multiple cell lines. SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 activity is unaffected by human serum. SNS-032 induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, SNS-032 induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 and dephosphorylated CDK7.
In vivo
SNS-032 prevents tumor cell-induced VEGF secretion in a tumor coculture model. SNS-032, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors.
Cell Data
cell lines:
Concentrations:0–0.5 mM
Incubation Time:24, 48, or 72 hours
Powder Purity:≥99%
Umfassendes Dokument zu Gefahren, Handhabung, Lagerung und Einhaltung regulatorischer Vorschriften.
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| Lot Number | Certificate Type | Datum | Artikel |
|---|---|---|---|
| Certificate of Analysis | Apr 03, 2026 | S407752 |
| Löslichkeit | Solubility (25°C) In vitro DMSO: 62 mg/mL (197.21 mM); Ethanol: 62 mg/mL (197.21 mM); Water: 2 mg/mL (6.36 mM); |
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