Ro492097
RO4929097
CAS: 847925-91-1
Molecular Formula: C22H20F5N3O3
Ro492097 - Names and Identifiers
Ro492097 - Physico-chemical Properties
| Molecular Formula | C22H20F5N3O3 |
| Molar Mass | 469.4 |
| Density | 1.40 |
| Boling Point | 696.3±55.0 °C(Predicted) |
| pKa | 12.35±0.46(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | Treatment of HEK293 cells with RO4929097 reduced the number of Aβ peptide secreted into the medium in A dose-dependent manner with an EC50 of 14 nM. In the Notch cell receptor assay, RO4929097 strongly inhibited the Notch program in a dose-dependent manner with an EC50 of 5 nM. Low nanomolar levels of RO4929097 are more than 100-fold more selective than 75 other different types of proteins (including receptors, ion channels, and enzymes) when used in cell-free and cell-based experiments. RO4929097 treatment of human NSCLC A549 cells for 5 days reduced ICN production and produced a less transformed tumor cell phenotype in tissue culture. RO4929097 acts on non-small cell lung cancer cells, inhibits the Notch program, and reduces the expression of Notch transcription target gene HES1. Treatment of SUM149 cells with RO4929097 reduced the expression of the direct Notch target genes Hes1, Hey1, and Heyl by 2-3 times, and in SUM190 cells by 3.5-8 times. RO4929097 slightly inhibited the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μm, RO4929097 acted on SUM149 and SUM190 cells, respectively, with growth inhibition rates of 20% and 10%, respectively, compared to the control group. PD4929097 reduces the production of inflammatory cytokines induced by T cells. Furthermore, treatment with RO4929097 caused a transition between TH2 and TH1 factors. In addition, PD4929097 increased T-cell activation-induced IL-6 production. Once RO4929097 treated selected melanoma cell lines, the NOTCH downstream effector HES1 was down-regulated. Once the primary melanoma cell line was treated with RO4929097, a decrease in the amount of melanospheres was detected. |
| In vivo study | RO4929097 treatment of A549 xenograft model, reduce the expression of genes associated with angiogenesis. In contrast, anti-ro4929097 H460a xenografts showed little change in these genes, highlighting the mechanism of RO4929097 anti-angiogenesis in vitro. RO4929097, administered orally to nude mice bearing A549 NSCLC xenografts at a dose of 3 to 60 mg/kg once or twice daily for 21 days, significantly inhibited tumor growth compared to controls. Tumor growth inhibition rates range from 66% to 91%. RO4929097 treated A549 tumors at a dose of 60 mg/kg twice daily on a 7 +/14-schedule initially caused tumor regression. At the end of the 21-day treatment schedule, tumor growth was still inhibited by 91% compared to the control group. After 34 days of treatment, the tumor growth inhibitory effect was delayed. On day 67 of the experiment, the same dose of PD4929097 was used for an additional 7 days. After treatment, it still has anti-cancer effect. RO4929097 acts on tumors that overexpress IL6 and IL8 and no longer affects angiogenesis or tumor-associated fibroblast infiltration. |
Ro492097 - Risk and Safety
| HS Code | 29242990 |
Ro492097 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.13 ml | 10.652 ml | 21.304 ml |
| 5 mM | 0.426 ml | 2.13 ml | 4.261 ml |
| 10 mM | 0.213 ml | 1.065 ml | 2.13 ml |
| 5 mM | 0.043 ml | 0.213 ml | 0.426 ml |
Last Update：2024-01-02 23:10:35
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CAS: 847925-91-1
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Product Name: RO4929097 Visit Supplier Webpage Request for quotation
CAS: 847925-91-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 847925-91-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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