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Briciclib {[allProObj[0].p_purity_real_show]}

货号:A265253 同义名: ON 014185

Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.

Briciclib 化学结构 CAS号:865783-99-9
Briciclib 化学结构
CAS号:865783-99-9
Briciclib 3D分子结构
CAS号:865783-99-9
Briciclib 化学结构 CAS号:865783-99-9
Briciclib 3D分子结构 CAS号:865783-99-9
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Briciclib 纯度/质量文件 产品仅供科研

货号:A265253 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cdc CDK1 CDK19 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CLK 其他靶点 纯度
XL413 hydrochloride ++++

Cdc7, IC50: 3.4 nM

99%+
SU9516 +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 22 nM

++

CDK4, IC50: 200 nM

99%+
RO-3306 +++

CDK1, Ki: 20 nM

SGK,ERK 98%
R547 ++++

CDK1/CyclinB, Ki: 2 nM

++++

CDK2/CyclinE, Ki: 3 nM

++++

CDK4/CyclinD1, Ki: 1 nM

99%+
BMS-265246 ++++

CDK1/CyclinB, IC50: 6 nM

++++

CDK2/CyclinE, IC50: 9 nM

+

CDK4/CyclinD, IC50: 230 nM

99%+
NU6027 +

CDK1, Ki: 2.5 μM

+

CDK2, Ki: 1.3 μM

DNA-PK 98%
Purvalanol A ++++

Cdc2/CyclinB, IC50: 4 nM

+++

CDK2/CyclinE, IC50: 35 nM

CDK2/CyclinA, IC50: 70 nM

+

CDK4/CyclinD1, IC50: 850 nM

99%+
SCH900776 ++

CDK2, IC50: 0.16 μM

99%+
AUZ 454 ++++

CDK2(C118L), Kd: 18.6 nM

CDK2(A144C), Kd: 9.7 nM

99%+
A-674563 HCl ++

CDK2, Ki: 46 nM

PKA 98%
JNJ-7706621 ++++

CDK1/CyclinB, IC50: 9 nM

++++

CDK2/CyclinE, IC50: 3 nM

CDK2/CyclinA, IC50: 4 nM

++

CDK3/CyclinE, IC50: 58 nM

+

CDK4/CyclinD1, IC50: 253 nM

++

CDK6/CyclinD1, IC50: 175 nM

99%+
AT7519 ++

CDK1/CyclinB, IC50: 210 nM

++

CDK2/CyclinA, IC50: 47 nM

+

CDK3/CyclinE, IC50: 360 nM

++

CDK4/CyclinD1, IC50: 100 nM

+++

CDK5/p35, IC50: 13 nM

++

CDK6/CyclinD3, IC50: 170 nM

++++

CDK9/CyclinT, IC50: <10 nM

98+%
PHA-793887 ++

CDK1/CyclinB, IC50: 60 nM

++++

CDK2/CyclinE, IC50: 8 nM

CDK2/CyclinA, IC50: 8 nM

++

CDK4/CyclinD1, IC50: 62 nM

++++

CDK5/p25, IC50: 5 nM

++++

CDK7/CyclinH, IC50: 10 nM

++

CDK9/CyclinT1, IC50: 138 nM

99%+
Milciclib +

CDK1/CyclinB, IC50: 398 nM

++

CDK2/CyclinE, IC50: 363 nM

CDK2/CyclinA, IC50: 45 nM

++

CDK4/CyclinD1, IC50: 160 nM

+

CDK5/p35, IC50: 265 nM

++

CDK7/CyclinH, IC50: 150 nM

99%+
Kenpaullone +

CDK1/CyclinB, IC50: 0.4μM

+

CDK2/CyclinE, IC50: 7.5μM

CDK2/CyclinA, IC50: 0.68μM

+

CDK5/p35, IC50: 0.85μM

98%
SNS-032 +++

CDK2/CyclinE, IC50: 48 nM

CDK2/CyclinA, IC50: 38 nM

+

CDK5/p35, IC50: 340 nM

++

CDK7/CyclinH, IC50: 62 nM

++++

CDK9/CyclinT, IC50: 4 nM

99%+
Dinaciclib ++++

CDK1, IC50: 3 nM

++++

CDK2, IC50: 1 nM

++++

CDK5, IC50: 1 nM

++++

CDK9, IC50: 4 nM

99%+
PHA-767491 hydrochloride ++++

Cdc7, IC50: 10 nM

+

CDK1, IC50: 250 nM

+

CDK2, IC50: 240 nM

+

CDK5, IC50: 460 nM

+++

CDK9, IC50: 34 nM

MK2 98%
(R)-Roscovitine +

Cdc2/CyclinB, IC50: 0.65 μM

+

CDK2/CyclinE, IC50: 0.7 μM

CDK2/CyclinA, IC50: 0.7 μM

++

CDK5/p35, IC50: 0.16 μM

99%+
Narazaciclib ++++

CDK4/CyclinD1, IC50: 3.87 nM

++++

CDK6/CyclinD1, IC50: 9.82 nM

RET 99%+
Palbociclib ++++

CDK4/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%
Abemaciclib ++++

CDK4, IC50: 2 nM

++++

CDK6, IC50: 10 nM

99%
Ribociclib ++++

CDK4, IC50: 10 nM

+++

CDK6, IC50: 39 nM

98%
Palbociclib isethionate ++++

CDK4/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%+
BS-181 HCl +++

CDK7, IC50: 21 nM

99%+
(E/Z)-THZ1 dihydrochloride ++++

CDK7, IC50: 3.2 nM

99%+
LDC4297 ++++

CDK7, IC50: 0.13 nM

99%+
Senexin A +

CDK19, Kd: 0.31 μM

+

CDK8, Kd: 0.83 μM

98+%
MSC2530818 ++++

CDK8, IC50: 2.6 nM

99%+
Wogonin 99%+
Riviciclib HCl ++

CDK1/CyclinB, IC50: 79 nM

+

CDK2/CyclinE, IC50: 2.54 μM

CDK2/CyclinA, IC50: 224 nM

++

CDK4/CyclinD1, IC50: 63 nM

+

CDK6/CyclinD3, IC50: 396 nM

+

CDK7/CyclinH, IC50: 2.87 μM

+++

CDK9/CyclinT1, IC50: 20 nM

99+%
LDC000067 +

CDK2, IC50: 2.441 μM

++

CDK9, IC50: 44 nM

98%
Flavopiridol +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 40 nM

+++

CDK4, IC50: 40 nM

+++

CDK6, IC50: 40 nM

+

CDK7, IC50: 300 nM

+++

CDK9, IC50: 20 nM

99%+
LY2857785 +

CDK7, IC50: 0.246 μM

+++

CDK8, IC50: 0.016 μM

+++

CDK9, IC50: 0.011 μM

99%+
AZD-5438 +++

CDK1, IC50: 16 nM

++++

CDK2, IC50: 6 nM

+++

CDK9, IC50: 20 nM

99%+
ML167 ++

Dyrk1B , IC50: 1648 nM

CLK4, IC50: 136 nM

99%+
(E/Z)-TG003 +++

mCLK1, IC50: 200 nM

mCLK4, IC50: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Briciclib 生物活性

描述 Briciclib targets eIF4E and inhibits the proliferation of various cancer cell lines including mantle cell leukemia, breast, gastric, and esophageal cancers with GI50 values of 9.8-12.2 nM, without affecting normal endothelial cells. It also reduces the expression of cyclin D1 and c-Myc in cancer cell lines within 8 hours[1].
体外研究

Briciclib targets eIF4E and inhibits the proliferation of various cancer cell lines including mantle cell leukemia, breast, gastric, and esophageal cancers with GI50 values of 9.8-12.2 nM, without affecting normal endothelial cells. It also reduces the expression of cyclin D1 and c-Myc in cancer cell lines within 8 hours[1].

Briciclib 参考文献

[1]Neel Jasani, et al. Abstract 1649: Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. Cancer Research. August 2015, Volume 75, Issue 15.

Briciclib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.54mL

2.11mL

1.05mL

21.08mL

4.22mL

2.11mL

Briciclib 技术信息

CAS号865783-99-9
分子式C19H23O10PS
分子量 474.419
别名 ON 014185
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 30 mg/mL(63.24 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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