905281-76-7
GDC-0879
CAS: 905281-76-7
Molecular Formula: C19H18N4O2
905281-76-7 - Names and Identifiers
905281-76-7 - Physico-chemical Properties
| Molecular Formula | C19H18N4O2 |
| Molar Mass | 334.37 |
| Density | 1.37 |
| Storage Condition | -20℃ |
| In vitro study | In vitro studies, The IC50 for GDC-0879 inhibition of MEK1 phosphorylation in V600E B- Raf mutated A375 melanoma and V600E B- Raf mutated Colo205 colon cancer cell lines were 59 and 29 nM, respectively. GDC-0879 effectively inhibited the B- raf V600E enzymatic action of Malme3M cells with an IC50 of 0.75 μm. With GDC-0879 treatment, cells with EC50 values <0.5 all expressed B- raf V600E oncogenic alleles (A375,624,SK-MEL-28,Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo 201). |
| In vivo study | GDC-0879 treated murine cell line and patient-derived B- raf V600E tumor showed stronger and longer lasting inhibitory effects (8 h treatment,>90%). And has higher viability compared to mutant KRAS-expressing tumors. Ras induced tumor formation with activated Raf signaling, but after treatment with GDC-0879, slow growth of some KRAS-mutated tumors was observed. The high efficiency of GDC-0879 regulation is completely related to the status of BRAF V600E, inhibiting MEK attenuates the growth and proliferation of tumors expressing wild-type B- raf. The responsiveness of BRAFV600E melanoma cells to GDC-0879 can be significantly altered by pharmacological and genetic modulation of PI3K pathway activity. |
905281-76-7 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.991 ml | 14.953 ml | 29.907 ml |
| 5 mM | 0.598 ml | 2.991 ml | 5.981 ml |
| 10 mM | 0.299 ml | 1.495 ml | 2.991 ml |
| 5 mM | 0.06 ml | 0.299 ml | 0.598 ml |
Last Update：2024-01-02 23:10:35
905281-76-7 - Reference Information
| biological activity | GDC-0879 (AR-00341677) is a new effective and selective B- Raf inhibitor. IC50 is 0.13 nM in A375 and Colo205 cells, which also has inhibitory effect on c-Raf. It has no inhibitory effect on other protein kinases. |
| target | TargetValue B- Raf (A375, Colo205 cells) 0.13 nM |
| Target | Value |
| B-Raf (A375, Colo205 cells) | 0.13 nM |
| in vitro study | in vitro study, in V600E B- Raf mutant A375 melanoma and V600E B- Raf mutant Colo205 colon cancer cell lines, the IC50 when GDC-0879 inhibits MEK1 phosphorylation was 59 and 29 nM respectively. GDC-0879 effectively inhibited the B- raf V600E enzymatic effect of Malme3M cells with IC50 of 0.75 μM. Cells with EC50 values <0.5 all expressed B- raf V600E oncogenic alleles (A375,624,SK-MEL-28,Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201) treated with GDC-0879. |
| In vivo studies | GDC-0879 treated mouse cell lines and patient-derived B- raf V600E tumors show stronger and more durable pharmacodynamic inhibition (treatment for 8 hours,>90%) and have higher viability compared with mutant KRAS-expressing tumors. Raf signal is activated when Ras induces tumor formation, but after treatment with GDC-0879, it is observed that the growth progression of some KRAS-mutant tumors is slow. The high efficiency of GDC-0879 regulation is completely related to the status of BRAFV600E. Inhibition of MEK weakens the growth and proliferation of wild-type B- raf tumors. Through the pharmacological and gene regulation of PI3K pathway activity, the reactivity of BRAFV600E melanoma cells to GDC-0879 can be obviously changed. |
Last Update：2024-04-09 22:09:11
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Product Name: GDC-0879 Visit Supplier Webpage Request for quotation
CAS: 905281-76-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 905281-76-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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