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

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

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Crozbaciclib Chemical Structure

Crozbaciclib Chemical Structure

CAS No. : 2099128-41-1

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Based on 1 publication(s) in Google Scholar

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Crozbaciclib Related Antibodies

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  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
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].

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

Crozbaciclib Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

488.57

Formula

C28H30F2N6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1(CCCC1)C2=CC(C3=NC(NC4=CC=C(C5CCN(C)CC5)C=N4)=NC=C3F)=C6)=NC2=C6F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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.
References
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Crozbaciclib Related Classifications

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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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HY-112280
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