Cat. No.: HY-111207

CA224

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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.

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Pureté: 99.94%
CAS No.: 883561-04-4
Formule: C₂₄H₂₂N₂O
Masse moléculaire:354.44

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CA224 Chemical Structure

CAS No.: 883561-04-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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)

Voir tous les produits spécifiques à Isoform CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.5 μM Compound: 1, CA224	Growth inhibition of p53+, pRb+ human A549 cells after 48 hrs by MTT assay Growth inhibition of p53+, pRb+ human A549 cells after 48 hrs by MTT assay	[PMID: 25368960]
A549	IC₅₀	3.5 μM Compound: CA224	Antiproliferative activity against A549 cells Antiproliferative activity against A549 cells	[PMID: 16750360]
Calu-1	IC₅₀	11.5 μM Compound: 1, CA224	Growth inhibition of p53 null, pRb+ human Calu1 cells after 48 hrs by MTT assay Growth inhibition of p53 null, pRb+ human Calu1 cells after 48 hrs by MTT assay	[PMID: 25368960]
Calu-1	IC₅₀	11.5 μM Compound: CA224	Antiproliferative activity against Calu1 cells Antiproliferative activity against Calu1 cells	[PMID: 16750360]
LS174T	IC₅₀	3.5 μM Compound: 1, CA224	Growth inhibition of p53+, pRb+ human LS 174T cells after 48 hrs by MTT assay Growth inhibition of p53+, pRb+ human LS 174T cells after 48 hrs by MTT assay	[PMID: 25368960]
LS174T	IC₅₀	3.5 μM Compound: CA224	Antiproliferative activity against LS174T cells Antiproliferative activity against LS174T cells	[PMID: 16750360]
NCI-H1299	IC₅₀	2.5 μM Compound: 1, CA224	Growth inhibition of p53 null, pRb+ human NCI-H1299 cells after 48 hrs by MTT assay Growth inhibition of p53 null, pRb+ human NCI-H1299 cells after 48 hrs by MTT assay	[PMID: 25368960]
NCI-H358	IC₅₀	2.2 μM Compound: 1, CA224	Growth inhibition of p53 null, pRb null human NCI-H358 cells after 48 hrs by MTT assay Growth inhibition of p53 null, pRb null human NCI-H358 cells after 48 hrs by MTT assay	[PMID: 25368960]
NCI-H460	IC₅₀	2 μM Compound: 1, CA224	Growth inhibition of p53+, pRb+ human NCI-H460 cells after 48 hrs by MTT assay Growth inhibition of p53+, pRb+ human NCI-H460 cells after 48 hrs by MTT assay	[PMID: 25368960]
PC-3	IC₅₀	6.2 μM Compound: 1, CA224	Growth inhibition of p53 null,pRb+ human PC3 cells after 48 hrs by MTT assay Growth inhibition of p53 null,pRb+ human PC3 cells after 48 hrs by MTT assay	[PMID: 25368960]
PC-3	IC₅₀	6.2 μM Compound: CA224	Antiproliferative activity against PC3 cells Antiproliferative activity against PC3 cells	[PMID: 16750360]
Sf9	IC₅₀	521 μM Compound: 2	Inhibition of human CDK2/GST-cyclin A expressed in Sf9 cells assessed as histone phosphorylation Inhibition of human CDK2/GST-cyclin A expressed in Sf9 cells assessed as histone phosphorylation	[PMID: 18650093]
Sf9	IC₅₀	6 μM Compound: 2	Inhibition of human CDK4/GST-cyclin D1 expressed in Sf9 cells assessed as retinoblastoma GST-RB152 phosphorylation Inhibition of human CDK4/GST-cyclin D1 expressed in Sf9 cells assessed as retinoblastoma GST-RB152 phosphorylation	[PMID: 18650093]

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.

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)
t_1/2,β (h)	0.33	1.16
AUC_0-t (ng·h/mL)	187	172
AUC_0-∞ (ng·h/mL)	189	182
C_{max (ng/mL)}	371	190
V_d (L/Kg)	2.52	nd
V_dss (L/Kg)	1.76	nd
CL (mL/min/kg)	88.3	nd
Bioavailability	-	9.6%
Time points considered for t_1/2,β calculation	0.5-2 h	1-4 h

Chemical Information

CAS No. 883561-04-4
Appearance Solid
Masse moléculaire 354.44
Formule C₂₄H₂₂N₂O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8214 mL

14.1068 mL

28.2135 mL

5 mM

0.5643 mL

2.8214 mL

5.6427 mL

10 mM

0.2821 mL

1.4107 mL

2.8214 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (286 KB)
SDS (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Sachin Mahale, et al. Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity. J Med Chem. 2014 Nov 26; [Content Brief]

[2]. Sachin Mahale, et al. CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4272-8.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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CA224

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CA224

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CA224 Related Classifications

HY-111207 Related Classifications