2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. CA224

CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.

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

CA224 Chemical Structure

CA224 Chemical Structure

CAS No. : 883561-04-4

Size Price Stock Quantity
1 mg USD 136 In-stock
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 768 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

CA224 Related Antibodies

Top Publications Citing Use of Products

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

CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity[1].

IC50 & Target

cdk4-cyclin D1

6.2 μM (IC50)

cdk2-cyclin A

521 μM (IC50)

In Vitro

CA224 (Compound 1) (48 h) shows antiproliferation activity against human cancer cell lines[1].
CA224 (18-48 h) blocks the growth of cancer cells at G0/G1 and G2/M phase of the cell cycle, and selectively kills SV40 large T-antigen transformed normal mouse embryonic liver cells (BNL SV A.8)[1][2].
CA224 (0-4 µM, 30 min) inhibits tubulin polymerization and enhances the depolymerization of stabilized tubulin protein[1].
CA224 (0-72 h) induces cell apoptosis in cancer cells[1].
CA224 (10 μM) shows 50%, 14%, 51% and 19% inhibition of CYP3A4, CYP2D6, CYP2C9, and CYP2C19, respectively[1].

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

CA224 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI-H1299, NCI-H358, BNL CL2 and BNL SV A.8
Concentration:
Incubation Time: 48 h
Result: Showed antiproliferation activity with IC50 values of 3.5, 6.2, 4.0, 3.5, 11.5, 2.0, 2.5, 2.2, 2.6 and 3.8 uM against LS174T, PC-3, MiaPaCa, A549, Calu-1, NCI-H460, NCI-H1299, NCI-H358, BNL CL2 and BNL SV A.8, respectively.

Cell Cycle Analysis[1][2]

Cell Line: A549, NCI-H1299, NCI-H358, BNL CL2, BNL SV A.8 and Calu-1
Concentration: IC50 concentration (IC70 for Calu-1)
Incubation Time: 24 h for A549, NCI-H1299 and Calu-1, 18 h for NCI-H358, 48 h for BNL CL2 and BNL SV A.8
Result: Induced a profound block at G2/M in A549 and NCI-H1299 cells. Maintained nocodazole- and paclitaxel-induced G2/M block in NCI-H358 cells. Exhibited prominent G2/M arrest in BNL CL2 cells. 31% of cells were detected in sub-G1 phase (control: 0%) in BNL SV A.8 cells. Retained the G0/G1 block in serum-starved p53-null Calu-1 cells.

Western Blot Analysis[1]

Cell Line: A549 and LS174T
Concentration: IC50 concentration; 1, 2, 3 and 4 µM for tubulin polymerization
Incubation Time: 24 h; 30 min for tubulin polymerization in A549 cells
Result: Induced p53, p21, and p27. Downregulated cyclin B1 and Cdk1. Inhibited tubulin polymerization in a dose-dependent manner and resulted in accumulation of unassembled tubulin in the supernatant.

Apoptosis Analysis[1]

Cell Line: A549, NCI-H460, NCI-H358, and NCI-H1299
Concentration: IC50 and IC70 concentration
Incubation Time: 24, 48 and 72 h
Result: Induces apoptotic cell death in a dose- and time-dependent manner.
In Vivo

CA224 (Compound 1) (100 mg/kg; i.p.; once a day for 9 days) shows significant tumor growth inhibition without obvious toxicity[1].

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

Animal Model: The severe combined immunodeficient (SCID) mouse, lacking both T and B immune cells. Male mice weighing 18−25 g, 6−8 weeks of age for subcutaneous injection of HCT-116, female mice weighing 15−24 g, 6−8 weeks of age for subcutaneous injection of NCI-H460[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection, once a day for 9 consecutive days
Result: Showed significant tumor growth inhibition in both HCT-116 and NCI-H460 tumor models without significant bodyweight loss.
Animal Model: BALB/c mice[1]
Dosage: 10 mg/kg (oral administration) or 1.0 mg/kg (intravenous injection)
Administration: Oral or intravenous injection (Pharmacokinetics Analysis)
Result: Pharmacokinetics parameters determined for CA224 after IV and PO administration[1].
Parameter IV (1 mg/kg) Oral (10 mg/kg)
t1/2,β (h) 0.33 1.16
AUC0-t (ng·h/mL) 187 172
AUC0-∞ (ng·h/mL) 189 182
Cmax (ng/mL) 371 190
Vd (L/Kg) 2.52 nd
Vdss (L/Kg) 1.76 nd
CL (mL/min/kg) 88.3 nd
Bioavailability - 9.6%
Time points considered
for t1/2,β calculation		 0.5-2 h 1-4 h
Molecular Weight

354.44

Formula

C24H22N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N(CCC3=CNC4=C3C=CC=C4)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (282.14 mM; Need ultrasonic; 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 2.8214 mL 14.1068 mL 28.2135 mL
5 mM 0.5643 mL 2.8214 mL 5.6427 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8214 mL 14.1068 mL 28.2135 mL 70.5338 mL
5 mM 0.5643 mL 2.8214 mL 5.6427 mL 14.1068 mL
10 mM 0.2821 mL 1.4107 mL 2.8214 mL 7.0534 mL
15 mM 0.1881 mL 0.9405 mL 1.8809 mL 4.7023 mL
20 mM 0.1411 mL 0.7053 mL 1.4107 mL 3.5267 mL
25 mM 0.1129 mL 0.5643 mL 1.1285 mL 2.8214 mL
30 mM 0.0940 mL 0.4702 mL 0.9405 mL 2.3511 mL
40 mM 0.0705 mL 0.3527 mL 0.7053 mL 1.7633 mL
50 mM 0.0564 mL 0.2821 mL 0.5643 mL 1.4107 mL
60 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1756 mL
80 mM 0.0353 mL 0.1763 mL 0.3527 mL 0.8817 mL
100 mM 0.0282 mL 0.1411 mL 0.2821 mL 0.7053 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CA224 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:

CA224883561-04-4CA 224CA-224CDKApoptosisCyclin dependent kinaseselectivefascaplysinantitumorLS174TPC-3A549Calu-1NCI-H460Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CA224
Cat. No.:
HY-111207
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.