1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. RGB-286147

RGB-286147 是一种选择性和 ATP 竞争性 CDKCDK 相关激酶 (CRK) 抑制剂,IC50 值范围为 9-839 nM。RGB-286147 对其他非 CDK/CRK 激酶的活性较低。RGB-286147 诱导细胞凋亡 (apoptosis),并具有抗肿瘤活性。

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RGB-286147 Chemical Structure

RGB-286147 Chemical Structure

CAS No. : 784211-09-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].

IC50 & Target[1]

CDK1/cyclinB

48 nM (IC50)

CDK2/E

15 nM (IC50)

CDK4/D1

839 nM (IC50)

cdk6/cyclin D3

232 nM (IC50)

体外研究
(In Vitro)

RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells[1].
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells[1].
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC50 value for inhibition of colony formation by RGB-286147 is 57 nM[1].
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 50 nM and 100 nM
Incubation Time: 24 or 48 hr
Result: Caused a marked inhibition of DNA replication and induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 100 nM
Incubation Time: 48 hr
Result: Resulted in proteolytic cleavage of PARP.
分子量

473.35

Formula

C23H22Cl2N4O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 30 mg/mL (63.38 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1126 mL 10.5630 mL 21.1260 mL
5 mM 0.4225 mL 2.1126 mL 4.2252 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.60%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1126 mL 10.5630 mL 21.1260 mL 52.8150 mL
5 mM 0.4225 mL 2.1126 mL 4.2252 mL 10.5630 mL
10 mM 0.2113 mL 1.0563 mL 2.1126 mL 5.2815 mL
15 mM 0.1408 mL 0.7042 mL 1.4084 mL 3.5210 mL
20 mM 0.1056 mL 0.5282 mL 1.0563 mL 2.6408 mL
25 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1126 mL
30 mM 0.0704 mL 0.3521 mL 0.7042 mL 1.7605 mL
40 mM 0.0528 mL 0.2641 mL 0.5282 mL 1.3204 mL
50 mM 0.0423 mL 0.2113 mL 0.4225 mL 1.0563 mL
60 mM 0.0352 mL 0.1761 mL 0.3521 mL 0.8803 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
RGB-286147
目录号:
HY-112346
需求量: