2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. CDK4/6-IN-10

CDK4/6-IN-10 是一种有效的、选择性的和具有口服活性的 CDK4 和 CDK6 抑制剂，其 IC50 值分别为 22 nM 和 10 nM。CDK4/6-IN-10 显示出抗肿瘤活性。CDK4/6-IN-10 具有研究多发性骨髓瘤 (MM) 的潜力。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

CDK4/6-IN-10 Chemical Structure

CDK4/6-IN-10 Chemical Structure

CAS No. : 2688098-11-3

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     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 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

CDK4/6-IN-10 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

CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM)[1].

IC50 & Target[1]

CDK4

22 nM (IC50)

CDK6/cyclinD1

10 nM (IC50)

体外研究
(In Vitro)

CDK4/6-IN-10 (compouns 32) (1 µM) shows kinase selectivity with IC50s of 22 nM and 10 nM for CDK4 and CDK6, respectively[1].
CDK4/6-IN-10 (72 h) shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 µM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively)[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1].
CDK4/6-IN-10 ( 0, 1, 2, 3 µM, 24 h) induces apoptosis of RPMI-8226 cells in a concentration-dependent manner[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) reduces the CDK4/6 activity by decreases the expression level of p-RB, c-MYC and BCL-2[1].

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

CDK4/6-IN-10 相关抗体:

Cell Proliferation Assay[1]

Cell Line: RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells
Concentration:
Incubation Time: 72 h
Result: Shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 µM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively).

Cell Cycle Analysis[1]

Cell Line: RPMI-8226 cells
Concentration: 0, 1.5, 3, 6 µM
Incubation Time: 24 h
Result: Cells were arrested at the G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: RPMI-8226 cells
Concentration: 0, 1.5, 3, 6 µM
Incubation Time: 24 h
Result: Reduced the CD4/K activity by decreased the expression level of p-RB, c-MYC and BCL-2.
体内研究
(In Vivo)

CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD50 much higher than 10,000 mg/kg[1].
CDK4/6-IN-10 (10 mg/kg; p.o.) shows oral bioavailability (F=51%) in SD rats[1].
CDK4/6-IN-10 (100, 200 mg/kg; p.o., once a day for 19 days) shows antitumor potency and favorable safety profile[1].
Pharmacokinetic Parameters of CDK4/6-IN-10 in SpragueeDawley rats[1].

Compd Admin. Cmax (ng/mL) AUC0-t (h·ng/mL) MRT0-t (h) Tmax (h) t1/2 (h) CL (mL/h/kg) F (%)
32 i.v. 355 960 5.9 0.033 8.9 641 -
p.o. 257 4,878 12.8 10.7 >24 524 51
SpragueeDawley rats, 10 mg/kg, p.o.

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

Animal Model: ICR mice[1]
Dosage: 1000, 5000, 10000 mg/kg
Administration: p.o.
Result: Showed safety profile with LD50 much higher than 10,000 mg/kg.
Animal Model: SpragueeDawley rats[1]
Dosage: 10 mg/kg
Administration: p.o.
Result: Showed oral bioavailability (F=51%).
Animal Model: BALB/c nude mice (6-8 weeks) (MM xenograft model)[1]
Dosage: 100, 200 mg/kg
Administration: p.o., once a day, 19 days
Result: Showed antitumor potency and favorable safety profile.
分子量

418.47

Formula

C22H23FN8
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.
纯度 & 产品资料
参考文献

CDK4/6-IN-10 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CDK4/6-IN-102688098-11-3CDKApoptosisCyclin dependent kinaseantitumorselectiveorally activeapoptosisxenograft modelRPMI-8226 cellsG1 phaseMultiple myelomasafety propertiesInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
CDK4/6-IN-10
目录号：
HY-115993
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z