Cat. No.: HY-144677

pan-HER-IN-2

Customer Review

Based on 1 Customer Validation

pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC₅₀ values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR^T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities.

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

Purity: 98.10%
CAS No.: 1639040-95-1
Formula: C₁₉H₁₅BrClN₅O
Molecular Weight:444.71

Storage:

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

pan-HER-IN-2 Chemical Structure

CAS No.: 1639040-95-1

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Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

EGFR

0.72 nM (IC₅₀)

HER4

2.0 nM (IC₅₀)

EGFR (L858R/T790M)

8.2 nM (IC₅₀)

HER2

75.1 nM (IC₅₀)

All EGFR Isoforms :

Chemical Information

CAS No. 1639040-95-1
Appearance Solid
Molecular Weight 444.71
Formula C₁₉H₁₅BrClN₅O
Color Light yellow to yellow
SMILES

O=C(NC1=CC=C2N=CN=C(C2=C1)NC3=CC4=C(NC=C4Br)C=C3)CCCl
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 (224.87 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

2.2487 mL

11.2433 mL

22.4866 mL

5 mM

0.4497 mL

2.2487 mL

4.4973 mL

10 mM

0.2249 mL

1.1243 mL

2.2487 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.62 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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)

References

[1]. Tang Q, et al. Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. Eur J Med Chem. 2022 Apr 5;233:114249. [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, 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	2.2487 mL	11.2433 mL	22.4866 mL	56.2164 mL
	5 mM	0.4497 mL	2.2487 mL	4.4973 mL	11.2433 mL
	10 mM	0.2249 mL	1.1243 mL	2.2487 mL	5.6216 mL
	15 mM	0.1499 mL	0.7496 mL	1.4991 mL	3.7478 mL
	20 mM	0.1124 mL	0.5622 mL	1.1243 mL	2.8108 mL
	25 mM	0.0899 mL	0.4497 mL	0.8995 mL	2.2487 mL
	30 mM	0.0750 mL	0.3748 mL	0.7496 mL	1.8739 mL
	40 mM	0.0562 mL	0.2811 mL	0.5622 mL	1.4054 mL
	50 mM	0.0450 mL	0.2249 mL	0.4497 mL	1.1243 mL
	60 mM	0.0375 mL	0.1874 mL	0.3748 mL	0.9369 mL
	80 mM	0.0281 mL	0.1405 mL	0.2811 mL	0.7027 mL
	100 mM	0.0225 mL	0.1124 mL	0.2249 mL	0.5622 mL

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pan-HER-IN-2

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MCE Bioactive Compound Library

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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

All EGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

pan-HER-IN-2 Related Classifications

HY-144677 Related Classifications