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PARP1/BRD4-IN-2
本半岛bd体育手机客户端 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。
PARP1/BRD4-IN-2图片
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
PARP1/BRD4-IN-2 是一种有效且具有选择性的 PARP1和 BRD4抑制剂， IC50分别为 197 nM 和 238 nM。PARP1/BRD4-IN-2 抑制 DNA 损伤修复，阻止 G0/G1 细胞周期转变，诱导细胞凋亡 ( apoptosis)。PARP1/BRD4-IN-2 在MDA-MB-468小鼠异种移植瘤模型中具有抗肿瘤活性。PARP1/BRD4-IN-2 可用于三阴性乳腺癌 (TNBC) 的研究。
生物活性

PARP1/BRD4-IN-2 is a potent and selectivePARP1andBRD4inhibitor withIC50values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and inducesapoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breastcancer(TNBC)[1].
IC50& Target[1]

BRD4

238 nM (IC50)

PARP1

197 nM (IC50)
体外研究
(In Vitro)

PARP1/BRD4-IN-2 (compound BP44) can directly bind to BRD4 and PARP1 in MDA-MB-468 cells and improve their thermal stability[1].
PARP1/BRD4-IN-2 has antiproliferative activity against MDA-MB-231 and MDA-MB-468 with IC50s of 6.61±0.58 μM and 3.01±0.83 μM, respectively[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates Bcl-2 and up-regulates Bax and cleaved caspase3 at 20 μM; inhibits colony formation and promotes cell apoptosis in MDA-MB-468 cells[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates DNA damage-related proteins CtIP, Mre11, Rad51, and p-RPA32 dose-dependently; causes DNA damage repair defects by down-regulating Rad51 and p-RPA32[1].
体内研究
(In Vivo)

PARP1/BRD4-IN-2 (40 and 80 mg/kg; IG, for 16 days) significantly inhibits tumor growth in xenograft mice and without significant toxicities, and significantly down-regulates the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues[1].
Pharmacokinetic Parameters of PARP1/BRD4-IN-2 in Sprague-Dawley rats[1].

IV (1 mg/kg) PO (10 mg/kg)
T1/2(h) 3.02 ± 0.57 3.33 ± 0.71
Cmax(ng/mL) 258 ± 11 242 ± 6
AUC0-t(ng/mL·h) 629 ± 49 1489 ± 130
AUC0-∞(ng/mL·h) 642 ± 36 1530 ± 146
VZ(L/kg) 21.1 ± 2.6
CL (mL/min/kg) 33.7 ± 1.5
F (%) 23.8 ± 1.3

Animal Model: Female BALB/c nude mice (implanted subcutaneously with MDA-MB-468 tumor cells)[1]
Dosage: 40 and 80 mg/kg
Administration: IG, for 16 days
Result: Significantly inhibited tumor growth and exhibits no significant toxicities; and significantly down-regulated the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues.
分子量

440.45
Formula

C25H20N4O4
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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