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| 货号： | IMA1042-0002MG |
| 保存条件： | -20℃ |
| CAS号： | 905281-76-7 |
| 供应商： | 上海伟进生物科技有限公司 |
| 数量： | 10 |
| 英文名： | GDC 0879 |
| 保质期： | 2 years |
| 规格： | 2mg |
Biological Activity
GDC-0879 is a potent, orally bioavailable and pyrazole-based class of ATP competitive inhibitor of B-Raf. The compound selectively inhibits purified B-Raf V600E enzyme with an IC50 estimate of 0.13 nM and a cellular pERK IC50 of 63 nM in the MALME-3M cell line [1].GDC-0879 displays comparable in vitro potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are V600E B-Raf mutant, with IC50 estimates of pMEK1 inhibition of 59 and 29 nM, respectively.GDC-0879 dose-dependently inhibits tumor growth both in A375 and Colo205 xenografts [2]. In GDC-0879-treated mice, both cell line- and patient- derived BRAFV600E tumors exhibits stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors. GDC-0879-induced signaling changes are dependent on the point of oncogenic activation within the RAS network [3].
Chemical Properties
| Cas No.: 905281-76-7 | M. Wt.: 334.37 |
| Formula: C19H18N4O2 | Purity: >99% |
| Synonym: GDC 0879, GDC0879, AR00341677 | |
| Chemical Name: 2-[4-[(1E)-1-(Hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol | |
| Appearance: White solid | |
| Solubility: Soluble to 100 mM in DMSO | |
| Storage：Store solid at -20 ºC desiccated | |
Application Concentration (Just for reference)
The appropriate working concentration of GDC-0879 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.
[VIP第1年] 指数:2
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