产品
编 号:F185818
分子式:C28H40BrN7O4
分子量:618.57
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10mM*1mL in DMSO
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1mg
240
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5mg
792
In-stock
10mg
1260
In-stock
50mg
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生物活性:
SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells.

体内研究:
SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors.Animal Model:Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model).
Dosage:10 mg/kg
Administration:Intraperitoneal injection; twice a week for 6 weeks.
Result:Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group).Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.

体外研究:
SGC0946 (0-100 μM; 4 days) inhibits DOT1L with IC50 of 2.65 nM in A431 cells.?SGC0946 (1, 5 μM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene).?SGC0946 (1 μM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation.?SGC0946 (1 μM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1.?SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity.?SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells.
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