Art. -Nr.: HY-150024

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BI-4142

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BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC₅₀ of 5 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.02%
CAS. Nr.: 2682003-36-5
Formel: C₂₈H₂₇N₉O₂
Molecular Weight:521.57

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

BI-4142 Chemical Structure

CAS. Nr.: 2682003-36-5

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Use of MCE Products

Antibody-Drug Conjugates

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

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

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC₅₀ of 5 nM^[1].

IC₅₀ & Target

HER2

5 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

In Vitro

BI-4142 shows inhibition with IC₅₀ values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2^YVMA, Ba/F3 HER2^YVMA, HEK EGFR^WT and Ba/F3 EGFR^WT, respectively^[1].
BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells^[1].
BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay^[1].
BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

NCI-H2170 HER2^WT, NCI-H2170 HER2^YVMA, A431 EGFR^WT, Ba/F3 HER2^YVMA, Ba/F3 HER2^YVMA,S783C, Ba/F3 EGFR^WT and Ba/F3 EGFR^C775S cells
Concentration:

1 nM-5 μM
Incubation Time:

72 h or 96 h
Result:

Showed antiproliferative effect with IC₅₀ values of 16 nM, 82 nM, >5 µM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2^WT, NCI-H2170 HER2^YVMA, A431 EGFR^WT, Ba/F3 HER2^YVMA, Ba/F3 HER2^YVMA,S783C, Ba/F3 EGFR^WT and Ba/F3 EGFR^C775S, respectively.

In Vivo

BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling^[1].

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

Animal Model:

NMRI-Foxn1nu mice, PC-9 HER2^YVMA xenograft model^[1]
Dosage:

3, 10, 30 and 100 mg/kg
Administration:

Oral administration, twice per day for 40 days
Result:

Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).

Animal Model:

BomTac:NMRI Foxn1nu mice^[1]
Dosage:

1 mg/kg or 10mg/kg and 100 mg/kg
Administration:

IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)

Result:

In vivo mouse PK data for BI-4142^[1]

Compound	Dose iv/po (mg/kg)	tmax (h)	C_max (nM)	AUD (h•nM)	Plasma CL (mL/min/kg)	% F
	i.v., 1mg/kg	n/a	n/a	3,280	9.69	n/a
BI-4142	p.o., 10 mg/kg	0.83	8,600	23,200	n/a	71
	p.o., 100 mg/kg	0.67	36,400	196,000	n/a	60

Chemical Information

CAS. Nr. 2682003-36-5
Appearance Solid
Molecular Weight 521.57
Formel C₂₈H₂₇N₉O₂
Color Light yellow to yellow
SMILES

O=C(N1CCN(CC1)C2=NC=C3N=CN=C(C3=N2)NC4=CC=C(C(C)=C4)OC5=CC(N=CN6C)=C6C=C5)C=C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (191.73 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

1.9173 mL

9.5864 mL

19.1729 mL

5 mM

0.3835 mL

1.9173 mL

3.8346 mL

10 mM

0.1917 mL

0.9586 mL

1.9173 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 (protect from 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

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

Solubility: 2.5 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (277 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]. Wilding B, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836. [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	1.9173 mL	9.5864 mL	19.1729 mL	47.9322 mL
	5 mM	0.3835 mL	1.9173 mL	3.8346 mL	9.5864 mL
	10 mM	0.1917 mL	0.9586 mL	1.9173 mL	4.7932 mL
	15 mM	0.1278 mL	0.6391 mL	1.2782 mL	3.1955 mL
	20 mM	0.0959 mL	0.4793 mL	0.9586 mL	2.3966 mL
	25 mM	0.0767 mL	0.3835 mL	0.7669 mL	1.9173 mL
	30 mM	0.0639 mL	0.3195 mL	0.6391 mL	1.5977 mL
	40 mM	0.0479 mL	0.2397 mL	0.4793 mL	1.1983 mL
	50 mM	0.0383 mL	0.1917 mL	0.3835 mL	0.9586 mL
	60 mM	0.0320 mL	0.1598 mL	0.3195 mL	0.7989 mL
	80 mM	0.0240 mL	0.1198 mL	0.2397 mL	0.5992 mL
	100 mM	0.0192 mL	0.0959 mL	0.1917 mL	0.4793 mL

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BI-4142

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer 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

Heterocyclic 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

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BI-4142 Related Classifications

HY-150024 Related Classifications