2. Cell Cycle/DNA Damage
  3. CDK
  4. Crozbaciclib

Crozbaciclib  (Synonyms: CDK4/6/1 Inhibitor)

目录号: HY-112280 纯度: 99.26%
COA 产品使用指南

摩尔计算器

Crozbaciclib (CDK4/6/1 Inhibitor) 是 CDK4/6 的抑制剂，IC50 值分别为 3 和 1 nM。

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Crozbaciclib Chemical Structure

Crozbaciclib Chemical Structure

CAS No. : 2099128-41-1

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Other Forms of Crozbaciclib:

Crozbaciclib 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

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.

IC50 & Target

IC50: 3 nM (CDK4), 1 nM (CDK6)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
U-87MG ATCC IC50
15.3 nM
Compound: 11
Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay
Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay
[PMID: 29247857]
体外研究
(In Vitro)

Crozbaciclib is a potent anti-proliferative agent that arrests U87MG cell line exclusively in G1 (IC50=15.3 ± 2.9 nM in the anti-proliferation assay). Crozbaciclib (13.72 nM; 24 h) significantly increases in the percentage of cells in G1 in U87MG cells[1].

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

Crozbaciclib 相关抗体:
体内研究
(In Vivo)

Crozbaciclib (3.125-50 mg/kg; ) has tumor growth inhibition values ranging from 62% to 99% in an orthotopic xenograft mouse model of glioblastoma multiforme. And Crozbaciclib results insignificant body weight loss. Crozbaciclib increases life span based on the median survival time of vehicle-treated animals in mice is significant at 162%, at a dose of 50 mg/kg[1].

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

488.57

Formula

C28H30F2N6
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
Cell Assay
[1]

The U87MG glioblastoma cells are treated with CDK4/6/1 and incubated for 72 h at 37°C. Then the medium is removed, 4% paraformaldehyde (50 µL/well) is added to the wells, and the cells are fixed for 30 min at RT. Cells are washed twice with phosphate-buffered saline (PBS) solution, and permeabilized in 0.2% Triton-X100 for 5 min. Cells are ished twice with PBS, after which 50 µL DAPI (1 µg/mL) is added to the wells, followed by incubation of the cells in the dark for 20 min. After ishing three times with PBS, PBS (100 µL/well) is added to the wells. The plates are scanned using IN Cell Analyzer 2200[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]

In the U87MG-Luc orthotopic xenograft mouse model, mice are treated with 3.125, 6.25, 12.5, 25, 50 mg/kg QD CDK4/6/1 Inhibitor for 28 days

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

Crozbaciclib 相关分类

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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:

Crozbaciclib2099128-41-1CDK4/6/1 InhibitorCDKCyclin dependent kinaseInhibitorinhibitorinhibit

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目录号：
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