XY221
XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
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- 화학식: C32H34FN3O5
- 분자량:559.63
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보관:
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Biological Activity
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Biological Activity
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BRD4 BD1 3869 nM (IC50) |
BRD4 BD2 5.8 nM (IC50) |
BRD3 BD2 70.98 nM (Ki) |
XY221 inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2, BRDT BD2 and BRD4 BD1 with IC50s of 5.8, 70.98, 53.47, 183, 3869 nM, respectively[1].
XY221 (72 h) inhibits MV4−11, LNCaP, HL-7702 cells proliferation with IC50s of 0.51, 0.68, 47.7 μM, respectively[1].
XY221 (500-2000 nM, 72 h) significantly induces antiproliferative activity and apoptosis in MV4−11 cell line[1].
XY221 (1-10 μM, 2h) displays long T1/2 (>120 min) in RLM (rat liver microsomes) and T1/2 (>120 min) in HLM (human liver microsomes)[1].
XY221 (500-2000 nM, 72h) inhibits target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK
in MV4−11 cells[1].
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XY221 (2 μM, 72h) suppresses oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level in MV4−11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4−11 cells
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Concentration:500, 2000 nM
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Incubation Time:24-72 h
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Result:Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.
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Cell Line:MV4−11 cells
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Concentration:2 μM
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Incubation Time:72 h
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Result:Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.
Suppressed oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level.
| route | Cmax(μg/L) | Tmax(h) | AUC(0-t)(μg/L・h) | AUC(0-∞)(μg/L・h) | T1/2(h) | CI(L/h/kg) | F (%) |
| iv (5 mg/kg) | 9790 | 0.03 | 4291 | 4294 | 1.35 | 1.21 | |
| po (25 mg/kg) | 567 | 3.67 | 2811 | 2816 | 2.13 | 13.1 |