2. Cell Cycle/DNA Damage
  3. CDK
  4. CGP-82996

GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。GP-82996 对 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35 的 IC50s 分别为 1.5、5.6 和 25 μM。GP-82996 诱导肿瘤细胞 U2OS 的凋亡 (apoptosis)。GP-82996可用于癌症研究。

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CGP-82996 Chemical Structure

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货
5 mg ￥960
询问价格 & 货期
10 mg ￥1520
询问价格 & 货期
25 mg ￥3104
询问价格 & 货期
50 mg ￥4960
询问价格 & 货期
100 mg ￥7840
询问价格 & 货期

* Please select Quantity before adding items.

Customer Review

CGP-82996 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

体外研究
(In Vitro)

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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

CGP-82996 相关抗体:
体内研究
(In Vivo)

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.
分子量

456.58

Formula

C27H32N6O
CAS 号
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.
溶解性数据

  • 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

In Vivo:

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

  • 方案 一

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline

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

只
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
参考文献

CGP-82996 相关分类

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.

Keywords:

CGP-82996359886-84-3CINK4CGP82996CGP 82996CINK 4CINK-4CDKCyclin dependent kinasecancerG1 arresthyperphosphorylation of pRbaooptosisKRAS mutationcellsInhibitorinhibitorinhibit

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产品名称：
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目录号：
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