Art. -Nr.: HY-19909

NRC-2694

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NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Reinheit: 99.84%
CAS. Nr.: 936446-61-6
Formel: C₂₄H₂₆N₄O₃
Molecular Weight:418.49

Speicherung:

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

NRC-2694 Chemical Structure

CAS. Nr.: 936446-61-6

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One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	<0.1 μM Compound: 49	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 32739648]
PC-9	IC₅₀	0.1 μM Compound: 49	Antiproliferative activity against human PC-9 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-9 cells assessed as cell growth inhibition incubated for 72 hrs by SRB assay	[PMID: 32739648]

In Vitro

NRC-2694 at 80 ng (190 nm) concentrations causes comparable inhibition of EGFR expression^[1].

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

In Vivo

In toxicity studies, the maximum tolerated dose of NRC-2694 in male and female mice is 2000 mg/kg (po). NRC-2694 (10 mg/kg) regresses the tumor in mice^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 936446-61-6
Appearance Solid
Molecular Weight 418.49
Formel C₂₄H₂₆N₄O₃
Color White to off-white
SMILES

COC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCCN4CCOCC4
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 : 250 mg/mL (597.39 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

2.3895 mL

11.9477 mL

23.8954 mL

5 mM

0.4779 mL

2.3895 mL

4.7791 mL

10 mM

0.2390 mL

1.1948 mL

2.3895 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 (4.97 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 (4.97 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 (4.97 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

Protokoll

Cell Assay^[1]

The in vitro invasiveness of H1299 and A549 cells in the presence of various concentrations of NRC compounds (as determined by MTT assay) is assessed using a modified Boyden chamber assay. Cells are treated with these compounds for 48 hr. 1×10⁶ cells are suspended in 600 μL of serum-free medium supplemented with 0.2% BSA and placed in the upper compartment of the transwell chambers coated with matrigel (0.7 mg/mL). The lower compartment of the chamber is filled with 200 μL of serum medium and the cells are allowed to migrate for 24 h. after incubation, the cells are fixed and stained with Hema-3 and quantified. The migrated cells are quantified as percent invasion.

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

Animal Administration^[1]

Mice: Nude mice are implanted with 2×10⁶ A549 cells in the right hind limb flank. Upon the observance of a tumour (>2 mm), mice are given oral or ip treatments of the test compounds including erlotinib HCl used as positive control. A dose of 100 mg/kg of erlotinib HCl is identified as the base line dose.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Ramanadham Jyothi Prasad, et al. 6-7,dialkoxy quinazoline derivatives useful for treatment of cancer related disorders. US 8143250 B2

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	2.3895 mL	11.9477 mL	23.8954 mL	59.7386 mL
	5 mM	0.4779 mL	2.3895 mL	4.7791 mL	11.9477 mL
	10 mM	0.2390 mL	1.1948 mL	2.3895 mL	5.9739 mL
	15 mM	0.1593 mL	0.7965 mL	1.5930 mL	3.9826 mL
	20 mM	0.1195 mL	0.5974 mL	1.1948 mL	2.9869 mL
	25 mM	0.0956 mL	0.4779 mL	0.9558 mL	2.3895 mL
	30 mM	0.0797 mL	0.3983 mL	0.7965 mL	1.9913 mL
	40 mM	0.0597 mL	0.2987 mL	0.5974 mL	1.4935 mL
	50 mM	0.0478 mL	0.2390 mL	0.4779 mL	1.1948 mL
	60 mM	0.0398 mL	0.1991 mL	0.3983 mL	0.9956 mL
	80 mM	0.0299 mL	0.1493 mL	0.2987 mL	0.7467 mL
	100 mM	0.0239 mL	0.1195 mL	0.2390 mL	0.5974 mL

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NRC-2694

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alkyne Compound Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NRC-2694 Related Classifications

HY-19909 Related Classifications