Art. -Nr.: HY-115840

ICL-CCIC-0019

Name: ICL-CCIC-0019
Brand: MedChemExpress
SKU: HY-115840
Price: 33.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Kundenbewertung

Based on 1 Customer Validation

ICL-CCIC-0019 is a CHKA inhibitor with a human IC₅₀ of 270 nM. ICL-CCIC-0019 blocks choline phosphorylation and phosphatidylcholine synthesis via the CDP-choline pathway. ICL-CCIC-0019 inhibits choline uptake, mitochondrial respiration, TCA cycle flux, de novo fatty acid synthesis, and mitochondrial membrane potential, while inducing G1 phase arrest, ER stress, caspase-dependent apoptosis, AMPK activation, glycolysis, acetate uptake, and mitochondrial network disruption. ICL-CCIC-0019 can be used for cancer research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 97.80%
CAS. Nr.: 936498-64-5
Formel: C₂₆H₄₄Br₂N₄
Molecular Weight:572.46

Speicherung:

-20°C, sealed storage, away from moisture and light

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

ICL-CCIC-0019 Chemical Structure

CAS. Nr.: 936498-64-5

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CHKA

270 nM (IC₅₀)

Alle AMPK Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI50	0.64 μM	Antiproliferative activity against human HCT-116 colorectal cancer cells with reported GI50 from Figure 1. Antiproliferative activity against human HCT-116 colorectal cancer cells with reported GI50 from Figure 1.	34371769
A549	GI50	0.38 μM	Antiproliferative activity against human A549 lung cancer cells with reported GI50 from Figure 1. Antiproliferative activity against human A549 lung cancer cells with reported GI50 from Figure 1.	34371769
Panel NCI-60 cells	GI50	1.12 μM	Antiproliferative activity against NCI-60 panel assessed as median GI50 after 72 hrs continuous exposure by SRB assay. Antiproliferative activity against NCI-60 panel assessed as median GI50 after 72 hrs continuous exposure by SRB assay.	27206796
Breast cancer cell line	GI50	0.627 μM	Antiproliferative activity against breast cancer cell lines assessed as median GI50 after 72 hrs continuous exposure by SRB assay. Antiproliferative activity against breast cancer cell lines assessed as median GI50 after 72 hrs continuous exposure by SRB assay.	27206796
Non-small cell lung cancer cells	GI50	0.751 μM	Antiproliferative activity against non-small cell lung cancer cell lines assessed as median GI50 after 72 hrs continuous exposure by SRB assay. Antiproliferative activity against non-small cell lung cancer cell lines assessed as median GI50 after 72 hrs continuous exposure by SRB assay.	27206796

In Vitro

Anti-cancerCarbohydrate MetabolismLipid MetabolismProtein/Amino Acid MetabolismApoptosisCell Cycle RegulationMitochondrial FunctionOxidative StressEndoplasmic Reticulum StressOthers

Anti-cancer

ICL-CCIC-0019 shows submicromolar GI₅₀ values in HCT-116 and A549 cells and 30-120 µM in normal MCF-10A and ST-T1B cells^[1].
ICL-CCIC-0019 (72 h) inhibits proliferation of HCT-116, A549, HepG2, and Caco-2 cells with a mean GI₅₀ of 0.5 µM^[1].
ICL-CCIC-0019 (72 h) inhibits proliferation across eight prostate and colon cancer cell lines with a mean GI₅₀ of 0.6 µM^[1].
ICL-CCIC-0019 (72 h) inhibits cancer cell growth with an NCI-60 median GI₅₀ of 1.12 μM^[2].

Anti-cancer

Carbohydrate Metabolism

Lipid Metabolism

Protein/Amino Acid Metabolism

ICL-CCIC-0019 (1-10 μM; 24 h) depletes PCho and rewires glycolysis/TCA metabolism in HCT116 cells^[2].

Anti-cancer

Lipid Metabolism

ICL-CCIC-0019 (0.98-10 μM; 1-6 h pre-incubation/pulse/chase) inhibits choline uptake and PCho/lipid labeling in HCT116 cells with an EC₅₀ of 0.98 μM^[2].

Apoptosis

Cell Cycle Regulation

Anti-cancer

ICL-CCIC-0019 (10 μM; 24-48 h) induces G1 arrest and apoptosis in HCT116 and other cancer cell lines^[2].

Lipid Metabolism

ICL-CCIC-0019 (10 µM) is a CHKA inhibitor with a reported Δ49N CHKA2 IC₅₀ of 0.27 µM and 53% CHKA inhibition at 10 µM^[1].

Mitochondrial Function

ICL-CCIC-0019 (0.25-10 μM; 24 h) suppresses mitochondrial respiration and activates AMPK in HCT116 cells, with citrate synthase depletion in A549 models^[2].

Oxidative Stress

Endoplasmic Reticulum Stress

Anti-cancer

ICL-CCIC-0019 (1-10 μM; 24-48 h) induces ER stress markers in HCT116 cells without ROS generation^[2].

Others

ICL-CCIC-0019 (50 µM; 1-2 h) is taken up by HCT-116 cells in a time-dependent manner and reaches approximately twofold higher intracellular levels than CK145 at 1-2 h^[1].
ICL-CCIC-0019 (50 µM; 4 h) is taken up by C4-2B prostate cancer cells with mean uptake of 24.9-34.1 % µg^-1 protein and uptake is independent of serum^[1].
ICL-CCIC-0019 (0.27-10 μM) inhibits CHKA with an IC₅₀ of 0.27 μM and shows low off-target kinase inhibition at 10 μM^[2].

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

Cell Cycle Analysis^[2]

Cell Line:

HCT116, HUH-7, and MDA-MB-468 cells
Concentration:

1 μM; 10 μM
Incubation Time:

24 h (G1 arrest); 48 h (sub-G1 and caspase-3/7 apoptosis)
Result:

Dose-dependently arrested cells in G1 after 24 h (2-fold increase at 10 μM) and increased the sub-G1 population 3.7-fold after 48 h.
Caspase-3/7-mediated apoptosis was seen after 48 h exposure to ICL-CCIC-0019 in HCT116, HUH-7, and MDA-MB-468 cells.

Western Blot Analysis^[2]

Cell Line:

HCT116 cells
Concentration:

1 μM; 10 μM
Incubation Time:

24 h; 48 h
Result:

Increased the expression of ER stress markers ATF4, IRE1α, HSP70, and HSP90.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC	T_1/2α	T_1/2β	V_z
Mice^[2]	10 mg/kg	i.p.	5.3 μM	5 min	79 μM·min	5.8 min	11 h	4.6 L/kg
Mice^[2]	10 mg/kg	p.o.	0.036 μM	30 min	3.0	10 min	56 h	/

In Vivo

Anti-cancer

ICL-CCIC-0019 (5 mg/kg; i.p.; once daily; days 1-3 followed by 11-day recovery) produces potent antitumor activity in HCT116 xenografts in female BALB/c nude mice^[2].
ICL-CCIC-0019 (10 mg/kg; i.p.; single dose) reduces tumor ¹⁸F-D4-FCH uptake and choline kinase flux in HCT116 xenografts in female BALB/c nude mice^[2].

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

Animal Model:

BALB/c nude (female, 6-8 weeks old)^[2]
Dosage:

5 mg/kg
Administration:

i.p.; once daily; days 1-3 followed by 11-day recovery period
Result:

Resulted in potent antitumor activity in HCT116 xenografts.

Animal Model:

BALB/c nude (female, 6-8 weeks old)^[2]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

In HCT116 xenografts, [18F]-D4-FCH AUC0-60 was 191.9 (%ID/mL)*min in vehicle-treated controls, 145.8 (%ID/mL)*min at 24 hours after ICL-CCIC-0019, 139.4 (%ID/mL)*min at 48 hours after ICL-CCIC-0019, and 187.7 (%ID/mL)*min at 6 hours after ICL-CCIC-0019.
Kinetic modeling showed that tumor Kr decreased by 73% at 24 hours and 75% at 48 hours compared with control.
Tumor Ki decreased after 48 hours.

Related Protocols :

Chemical Information

CAS. Nr. 936498-64-5
Appearance Solid
Molecular Weight 572.46
Formel C₂₆H₄₄Br₂N₄
Color White to off-white
SMILES

CN(C)C1=CC=[N+](C=C1)CCCCCCCCCCCC[N+]2=CC=C(C=C2)N(C)C.[Br-].[Br-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture and light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 8.33 mg/mL (14.55 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

1.7468 mL

8.7342 mL

17.4685 mL

5 mM

0.3494 mL

1.7468 mL

3.4937 mL

10 mM

0.1747 mL

0.8734 mL

1.7468 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.83 mg/mL (1.45 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.83 mg/mL (1.45 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 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 (8.3 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Wang N, et al. Novel Non-Congeneric Derivatives of the Choline Kinase Alpha Inhibitor ICL-CCIC-0019. Pharmaceutics. 2021 Jul 14;13(7):1078.

[2]. Trousil S, et al. The novel choline kinase inhibitor ICL-CCIC-0019 reprograms cellular metabolism and inhibits cancer cell growth. Oncotarget. 2016 Jun 14;7(24):37103-37120. [Content Brief]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7468 mL	8.7342 mL	17.4685 mL	43.6712 mL
	5 mM	0.3494 mL	1.7468 mL	3.4937 mL	8.7342 mL
	10 mM	0.1747 mL	0.8734 mL	1.7468 mL	4.3671 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

ICL-CCIC-0019

Alle AMPK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen