Crozbaciclib (Synonyms: CDK4/6/1 Inhibitor)

Name: Crozbaciclib
Brand: MedChemExpress
SKU: HY-112280
Rating: 4.5 (1 reviews)

Cat. No.: HY-112280 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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

For research use only. We do not sell to patients.

Crozbaciclib Chemical Structure

CAS No. : 2099128-41-1

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
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10 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Crozbaciclib:

Crozbaciclib fumarate Get quote

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Biological Activity
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]

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]

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.

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.

2099128-41-1

Appearance

Solid

Color

Off-white 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

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (68.22 mM; ultrasonic and adjust pH to 3 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0468 mL	10.2339 mL	20.4679 mL
5 mM	0.4094 mL	2.0468 mL	4.0936 mL
10 mM	0.2047 mL	1.0234 mL	2.0468 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (249 KB) HNMR (262 KB) RP-HPLC (246 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28. [Content Brief]

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	[1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0468 mL	10.2339 mL	20.4679 mL	51.1697 mL
	5 mM	0.4094 mL	2.0468 mL	4.0936 mL	10.2339 mL
	10 mM	0.2047 mL	1.0234 mL	2.0468 mL	5.1170 mL
	15 mM	0.1365 mL	0.6823 mL	1.3645 mL	3.4113 mL
	20 mM	0.1023 mL	0.5117 mL	1.0234 mL	2.5585 mL
	25 mM	0.0819 mL	0.4094 mL	0.8187 mL	2.0468 mL
	30 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL
	40 mM	0.0512 mL	0.2558 mL	0.5117 mL	1.2792 mL
	50 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0234 mL
	60 mM	0.0341 mL	0.1706 mL	0.3411 mL	0.8528 mL

Crozbaciclib Related Classifications

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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Crozbaciclib (Synonyms: CDK4/6/1 Inhibitor)

Customer Review

Other Forms of Crozbaciclib:

Crozbaciclib Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Crozbaciclib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Crozbaciclib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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