Art. -Nr.: HY-109084

Conteltinib

(Synonyms: CT-707)

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Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC₅₀ of 1.6 nM.

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Reinheit: 99.0%
CAS. Nr.: 1384860-29-0
Formel: C₃₂H₄₅N₉O₃S
Molecular Weight:635.82

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Conteltinib Chemical Structure

CAS. Nr.: 1384860-29-0

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

Biologische Aktivität

Beschreibung

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC₅₀ of 1.6 nM^[1].

IC₅₀ & Target

IC50: 1.6 nM (FAK)^[1]

In Vitro

Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation^[1].
The combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone^[1].
The combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines^[1].
The FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184^[1].

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

Cell Viability Assay^[1]

Cell Line:

The human hepatocellular carcinoma cell lines HepG2 and Bel-7402
Concentration:

1.0, 1.5, 2.0, 2.5, and 3.0 μM for HepG2 cells; 0.2, 0.4, 0.8, 1.5, and 3.0 μM for Bel-7402 cells
Incubation Time:

72 hours
Result:

When cells were exposed to XL184 (5 μM), Conteltinib (3 μM), or their combination, the survival rates were 57.3%, 39.3%, and 11.2%, respectively, in HepG2; those in Bel-7402 were 57.8%, 61.6%, and 34.2%, respectively.

Apoptosis Analysis^[1]

Cell Line:

HepG2 and Bel-7402 cells
Concentration:

3 μM
Incubation Time:

48 hours
Result:

The apoptosis rates of control, XL184, Conteltinib, and combination groups in HepG2 were 5.0%, 10.5%, 18.4%, and 41.1%, respectively, and those in Bel-7402 were 4.4%, 16.3%, 8.7%, and 36.4%, respectively.

Western Blot Analysis^[1]

Cell Line:

HepG2 and Bel-7402
Concentration:

3 μM
Incubation Time:

24 hours
Result:

Could markedly decrease FAK phosphorylation induced by XL184, which might partially account for the synergetic effect.

In Vivo

The combination of XL184 (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707 (i.g. 50 mg/kg twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day) shows the synergistic antitumor effect in HepG2 xenograft nude mice^[1].

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

Animal Model:

Nude mice transplanted with HepG2 xenografts^[1]
Dosage:

50 mg/kg
Administration:

Intragastrically (i.g.) twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day.
Result:

Caused a moderate decrease in the relative tumor volume (RTV).
The inhibition rate of combination group reached 77.4%, whereas the mono-treatment of XL184 or CT-707 alone caused 30.7% and 19.4% inhibition in the tumor weight, respectively.

Chemical Information

CAS. Nr. 1384860-29-0
Appearance Solid
Molecular Weight 635.82
Formel C₃₂H₄₅N₉O₃S
Color Light yellow to yellow
SMILES

O=S(C1=C(C=CC=C1)NC2=C(CCN3)C3=NC(NC(C=CC(N4CCC(N5CCN(C)CC5)CC4)=C6)=C6OC)=N2)(NC(C)C)=O
Synonyms

CT-707
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 31.25 mg/mL (49.15 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

1.5728 mL

7.8639 mL

15.7277 mL

5 mM

0.3146 mL

1.5728 mL

3.1455 mL

10 mM

0.1573 mL

0.7864 mL

1.5728 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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 (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 DD, et al. CT-707, a Novel FAK Inhibitor, Synergizes with XL184 to Suppress Hepatocellular Carcinoma by Blocking XL184-Induced FAK Activation. Mol Cancer Ther. 2016 Dec;15(12):2916-2925. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5728 mL	7.8639 mL	15.7277 mL	39.3193 mL
	5 mM	0.3146 mL	1.5728 mL	3.1455 mL	7.8639 mL
	10 mM	0.1573 mL	0.7864 mL	1.5728 mL	3.9319 mL
	15 mM	0.1049 mL	0.5243 mL	1.0485 mL	2.6213 mL
	20 mM	0.0786 mL	0.3932 mL	0.7864 mL	1.9660 mL
	25 mM	0.0629 mL	0.3146 mL	0.6291 mL	1.5728 mL
	30 mM	0.0524 mL	0.2621 mL	0.5243 mL	1.3106 mL
	40 mM	0.0393 mL	0.1966 mL	0.3932 mL	0.9830 mL

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Conteltinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Conteltinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Conteltinib Related Classifications

HY-109084 Related Classifications