B026 是一种具有选择性且口服有效的 p300/CBP 组蛋白乙酰转移酶 (p300/CBP HAT) 抑制剂，对于 p300 和 CBP 的IC50值为 1.8 nM 和 9.5 nM。B026 对雄激素受体阳性 (AR+) 前列腺癌细胞具有抗癌活性。
| 生物活性 | B026 is a selective, potent, orally activep300/CBPhistone acetyltransferase(HAT)inhibitor withIC50values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostatecancercell lines[1]. |
体外研究
(In Vitro) | B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity[1].
B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression[1].
B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner[1].
B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP[1].
Cell Viability Assay[1] | Cell Line: | Maver-1, MV-4-11, K562, Kasumi-1, LnCaP-FGC and 22Rv1 cells | | Concentration: | 0-5 μM | | Incubation Time: | 12 hours | | Result: | Inhibited cell growth with IC50values of 2.6, 4.2, 4.4, 9.8, 40.5 and 104.4 nM for Maver-1, MV-4-11, 22Rv1, LnCaP-FGC, Kasumi-1 and K562 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | MV-4-11 cells | | Concentration: | 0, 0.313, 0.625, 1.25, 2.5 and 5 μM | | Incubation Time: | 6 hours | | Result: | Decreased the expression of H3K27Ac in a dose-dependent manner. |
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体内研究
(In Vivo) | B026 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat[1].
B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner[1].
| Animal Model: | Balb/c female mice with MV-4-11 xenograft[1] | | Dosage: | 50 and 100 mg/kg | | Administration: | Oral administration; daily, for 28 days | | Result: | Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively. |
| Animal Model: | Male SD rats[1] | | Dosage: | 1 and 3 mg/kg | | Administration: | Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours | | Result: | 1.19|
| Administration | i.v. (1 mg/kg) | p.o. (3 mg/kg) | | T1/2(h) | 1.5 | 1.02 | | Tmax(h) | | 0.83 | | Cmax(μM) | | 1.12 | | AUClast(μM·h) | 2.22 | 3.71 | | Vdss(L/kg) | 1.5 | | | CL_obs(mL/min/kg) | 13.4 | | | PPB % | | 98.2 | |
| F % | | 56 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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