| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
Cell lines | A549, HCT116, HT29 and MDAMB231 cancer cell lines |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 ℃ for several months. |
Reaction Conditions | 5 μM |
Applications | In all cell lines, RAF265 induced a decrease in clonogenic survival. In A549 cells, the combination of RAD001 and RAF265 enhanced the antiproliferative effect of RAF265. |
Animal models | Mice bearing H460 xenografts |
Dosage form | 12 mg/kg, p.o.; q.d. |
Applications | In mice bearing H460 xenografts, RAD001 and RAF265 given alone showed limited effect on inhibition of tumor growth. When combined with RAD001, RAF265 significantly delayed tumor growth. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| 产品描述 | RAF265, also known as CHIR-265, is a novel and orally available small molecule inhibitor of multiple intracellular kinases, including BRAFV600E, BRAF (wild-type), c-RAF, vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF) 1R, RET, c-KIT, SRC and STE20, with half maximal inhibitory concentration IC50 ranging from less than 20 nmo/L to more than 100 nmol/L, in which it exhibits the highest potency for BRAFV600E and VEGFR2 with half maximal effective concentration EC50 of 0.14 μM and 0.19 μM respectively. RAF265 has been found to inhibit proliferation of melanoma and colorectal cancer cell lines with active BRAF mutations and time- and dose-dependently suppress tumor regression in BRAFV600E melanoma and colorectal cancer xenograft models. References: |
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