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Cobimetinib GDC-0973 934660-93-2
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C21H21F3IN3O2 |
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531.31 |
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934660-93-2 |
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98%+ |
Introduction
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.
GDC-0973 shows strong cellular potency in a broad panel of tumor types, particularly in BRAF (with most of EC50 below 2 μM) or KRAS mutant cancer cell lines. In a panel of cancer cell lines, 80% of BRAF mutant lines (including V600E and non-V600E mutations) are sensitive to GDC-0973, 54% of lines carrying oncogenic mutations in KRAS or NRAS are sensitive, and 35% of the remaining lines are sensitive. GDC-0941 and GDC-0973 act cooperatively to inhibit the viability of all melanoma cell lines tested, 60% of which carry oncogenic mutations in BRAF. Combination of GDC-0941(0.2 μM) and GDC-0973 (10 μM) almost completely suppresses the vitality of 888MEL (BRAFV600E) mutant melanoma cell lines at 4 day. Treatment with GDC-0973 and GDC-0941 results in a combinatorial increase of cellular mediators of apoptosis, such as cleaved PARP and alternatively spliced isoforms of Bim. Transient treatment of 888MEL cells with either single agent GDC-0973 or GDC-0941 results in minimal to no apoptosis induction, whereas GDC-0973 plus GDC-0941 results in a 5-fold increase in apoptosis.
GDC-0973 shows strong cellular potency in a broad panel of tumor types, particularly in BRAF (with most of EC50 below 2 μM) or KRAS mutant cancer cell lines. In a panel of cancer cell lines, 80% of BRAF mutant lines (including V600E and non-V600E mutations) are sensitive to GDC-0973, 54% of lines carrying oncogenic mutations in KRAS or NRAS are sensitive, and 35% of the remaining lines are sensitive. GDC-0941 and GDC-0973 act cooperatively to inhibit the viability of all melanoma cell lines tested, 60% of which carry oncogenic mutations in BRAF. Combination of GDC-0941(0.2 μM) and GDC-0973 (10 μM) almost completely suppresses the vitality of 888MEL (BRAFV600E) mutant melanoma cell lines at 4 day. Treatment with GDC-0973 and GDC-0941 results in a combinatorial increase of cellular mediators of apoptosis, such as cleaved PARP and alternatively spliced isoforms of Bim. Transient treatment of 888MEL cells with either single agent GDC-0973 or GDC-0941 results in minimal to no apoptosis induction, whereas GDC-0973 plus GDC-0941 results in a 5-fold increase in apoptosis.