2. Cell Cycle/DNA Damage
  3. CDK
  4. AG-024104

AG-024104 是一种 CDK 抑制剂，针对 CDK1/cyclinB、CDK2/cyclinA 和 CDK4/cyclinD 的 Ki 值分别为 2.3 nM、1.8 nM 和 0.67 nM。AG-024104 可在功能上抑制 CDK1/cyclinB、CDK2/cyclinA 和 CDK4/cyclinD 的激酶活性。AG-024104 可作为临床前研究中外周白细胞毒性实验的阴性对照。

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AG-024104

AG-024104 Chemical Structure

CAS No. : 750575-23-6

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AG-024104 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development[1].

体外研究
(In Vitro)

AG-024104 可强效抑制纯化的 CDK1/cyclinB、CDK2/cyclinA 及 CDK4/cyclinD 酶，其 Ki 值分别为 2.3 nM、1.8 nM 和 0.67 nM[1]。
AG-024104 (连续给药 4 天) 可抑制 HCT-116 结直肠癌细胞的生长，其 IC50 为 51 nM[1]。
AG-024104 (给药 24 小时) 可诱导人 PBMC 和猴 PBL 产生细胞毒性，其 TC50 值分别为 7.2 μM 和 4.0 μM[1]。

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

AG-024104 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-116 colorectal carcinoma cells
Concentration: concentrations to achieve 50% growth inhibition (IC50 determination)
Incubation Time: 4 days
Result: Inhibited HCT-116 cell growth with an IC50 of 51 nM.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-24 T1/2
Rat[1] 10 mg/kg i.v. 2.7 μg·h/mL 1.4 h
体内研究
(In Vivo)

AG-024104 (单次静脉推注，时长 2-3 分钟，剂量 10 mg/kg) 不会对雄性 Sprague Dawley 大鼠的外周血白细胞计数产生显著的急性抑制作用，给药后 24 小时其白细胞计数仍维持在给药前水平的约 93%[1]。

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

Animal Model: Sprague Dawley (male, ~10 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.v.; single bolus injection over 2-3 min
Result: Remained at ~93% of pre-treatment levels 24 hours post-dose.
分子量

566.64

Formula

C24H28F2N6O4S2
CAS 号
中文名称

帕沙米特
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

AG-024104 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

AG-024104750575-23-6帕沙米特AG024104AG 024104CDKCyclin dependent kinaselymphocytesCDK4/cyclinDCDK1/cyclinBnude mouse xenograft modelsHCT-116 colorectal carcinoma cellmonkey peripheral blood mononuclear cellsSprague Dawley ratscolorectal carcinoma cellsCDK2/cyclinAhuman peripheral blood mononuclear cellsInhibitorinhibitorinhibit

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AG-024104
目录号：
HY-123238
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