1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK2/4/6-IN-1

CDK2/4/6-IN-1 (example 29) 是一种 CDK2/4/6 抑制剂,作用于 CDK2、CDK4、CDK6 的 IC50 值分别是 2.5、23.7 和 44.3 nM。可用于癌症研究。CDK2/4/6-IN-1 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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CDK2/4/6-IN-1 Chemical Structure

CDK2/4/6-IN-1 Chemical Structure

CAS No. : 2803837-13-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research[1]. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

CDK2

2.5 nM (IC50)

CDK4

23.7 nM (IC50)

CDK6

44.3 nM (IC50)

体外研究
(In Vitro)

CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits the proliferation of OVCAR3 and MCF7 cells with the IC50 values of 14.6 and 117.8 nM, respectively[1].
CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits phosphorylation of Rb protein in OVCAR3 and MCF7 cells with the IC50 values of 18 and 581 nM, respectively[1].

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

体内研究
(In Vivo)

CDK2/4/6-IN-1(example 29) (25 mg/kg or 50 mg/kg, once a day, orally) has a significant inhibitory effect on tumor growth[1].
The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.)

Parameters Cmax(ng/mL) Tmax(hr) AUClast(hr*ng/mL) T1/2(hr)
PO 4050 0.5 10050 4.8
The pharmacokinetic parameters of example 29 in BALB/c mice (3 mg/kg, i.v.)
Parameters C0(ng/mL) T1/2(hr) AUClast(hr*ng/mL) Vss(L/Kg)
IV 4407 0.7 3245 0.9

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

分子量

438.50

Formula

C22H22N4O4S

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
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  • 稀释计算器

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质量   浓度   体积   分子量 *
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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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  • 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:
CDK2/4/6-IN-1
目录号:
HY-148213
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