Crozbaciclib fumarate

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

Cat. No.: HY-112280A Purity: 99.37%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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

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

Crozbaciclib fumarate Chemical Structure

CAS No. : 2567494-39-5

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Crozbaciclib fumarate:

Crozbaciclib Get quote

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View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

Crozbaciclib fumarate 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 fumarate 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 fumarate (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 fumarate (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 fumarate results insignificant body weight loss. Crozbaciclib fumarate 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

604.65

Formula

C₃₂H₃₄F₂N₆O₄

CAS No.

2567494-39-5

Appearance

Solid

Color

White to yellow

SMILES

CC(C1(CCCC1)C2=CC(C3=NC(NC4=CC=C(C5CCN(C)CC5)C=N4)=NC=C3F)=C6)=NC2=C6F.OC(/C=C/C(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (82.69 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6538 mL	8.2692 mL	16.5385 mL
5 mM	0.3308 mL	1.6538 mL	3.3077 mL
10 mM	0.1654 mL	0.8269 mL	1.6538 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.37%

Select Batch:

Data Sheet (269 KB) SDS (252 KB)

COA (246 KB) HNMR (253 KB) RP-HPLC (238 KB) LCMS (98 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]

Complete Stock Solution Preparation Table

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

H₂O	1 mM	1.6538 mL	8.2692 mL	16.5385 mL	41.3462 mL
	5 mM	0.3308 mL	1.6538 mL	3.3077 mL	8.2692 mL
	10 mM	0.1654 mL	0.8269 mL	1.6538 mL	4.1346 mL
	15 mM	0.1103 mL	0.5513 mL	1.1026 mL	2.7564 mL
	20 mM	0.0827 mL	0.4135 mL	0.8269 mL	2.0673 mL
	25 mM	0.0662 mL	0.3308 mL	0.6615 mL	1.6538 mL
	30 mM	0.0551 mL	0.2756 mL	0.5513 mL	1.3782 mL
	40 mM	0.0413 mL	0.2067 mL	0.4135 mL	1.0337 mL
	50 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8269 mL
	60 mM	0.0276 mL	0.1378 mL	0.2756 mL	0.6891 mL
	80 mM	0.0207 mL	0.1034 mL	0.2067 mL	0.5168 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.