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B026
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
B026图片
CAS NO:2379416-48-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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.
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
Administrationi.v. (1 mg/kg)p.o. (3 mg/kg)
T1/2(h)1.51.02
Tmax(h)0.83
Cmax(μM)1.12
AUClast(μM·h)2.223.71
Vdss(L/kg)1.5
CL_obs(mL/min/kg)13.4
PPB %98.2
F %56
分子量

557.50

Formula

C27H23F4N5O4

CAS 号

2379416-48-3

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.