Cat. No.: HY-150023

BI-1622

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BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC₅₀ of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.

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

Purity: 98.02%
CAS No.: 2681392-19-6
Formula: C₂₆H₂₄N₁₀O₂
Molecular Weight:508.53

Storage:

4°C, protect from light

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

BI-1622 Chemical Structure

CAS No.: 2681392-19-6

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(In Japan)

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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
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

HER2

7 nM (IC₅₀)

ErbB4

EGFR

CDK11B

JAK3

All EGFR Isoforms :

All PI4K Isoforms :

All CDK Isoforms :

All Raf Isoforms :

All JAK Isoforms :

In Vitro

BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines^[1].
BI-1622 induces a dose-dependent decrease in pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells with an accompanying decrease in DUSP6 messenger RNA levels^[1].
BI-1622 displays good permeability and no PgP-mediated efflux liability^[1].
BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Ba/F3 cells
Concentration:

0-5 µM
Incubation Time:

72 h or 96 h
Result:

Potently inhibited the proliferation of cancer cell lines dependent on amplified HER2 or an NRG-1 fusion. Inhibited different HER2 oncogenic variants and HER2WT with IC₅₀ values below 50 nM in tumor cell lines, while sparing EGFRWT-driven cells.

In Vivo

BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability^[1].
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo^[1].

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

Animal Model:

Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)^[1]
Dosage:

10, 30 and 100 mg/kg
Administration:

orally, twice daily
Result:

In the NCI-H2170 HER2YVMA mechanistic model, 100 mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100 mg/kg twice daily) resulted in tumor regressions.

Animal Model:

NMRI Foxn1nu mice (n=3 per group)^[1]
Dosage:

1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration:

IV, Orally; once (Pharmacokinetic Analysis)
Result:

Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.

Chemical Information

CAS No. 2681392-19-6
Appearance Solid
Molecular Weight 508.53
Formula C₂₆H₂₄N₁₀O₂
Color Light yellow to yellow
SMILES

O=C(N1CCN(CC1)C2=NC3=C(NC4=CC=C(C(C)=C4)OC5=CC6=NC=NN6C=C5)N=CN=C3C=N2)C=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (196.65 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

1.9665 mL

9.8323 mL

19.6645 mL

5 mM

0.3933 mL

1.9665 mL

3.9329 mL

10 mM

0.1966 mL

0.9832 mL

1.9665 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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)
- 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)

References

[1]. Lamarre L, 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	1.9665 mL	9.8323 mL	19.6645 mL	49.1613 mL
	5 mM	0.3933 mL	1.9665 mL	3.9329 mL	9.8323 mL
	10 mM	0.1966 mL	0.9832 mL	1.9665 mL	4.9161 mL
	15 mM	0.1311 mL	0.6555 mL	1.3110 mL	3.2774 mL
	20 mM	0.0983 mL	0.4916 mL	0.9832 mL	2.4581 mL
	25 mM	0.0787 mL	0.3933 mL	0.7866 mL	1.9665 mL
	30 mM	0.0655 mL	0.3277 mL	0.6555 mL	1.6387 mL
	40 mM	0.0492 mL	0.2458 mL	0.4916 mL	1.2290 mL
	50 mM	0.0393 mL	0.1966 mL	0.3933 mL	0.9832 mL
	60 mM	0.0328 mL	0.1639 mL	0.3277 mL	0.8194 mL
	80 mM	0.0246 mL	0.1229 mL	0.2458 mL	0.6145 mL
	100 mM	0.0197 mL	0.0983 mL	0.1966 mL	0.4916 mL

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BI-1622

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism 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

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target 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

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

All EGFR Isoforms

All PI4K Isoforms

All CDK Isoforms

All Raf Isoforms

All JAK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BI-1622 Related Classifications

Cat. No.: HY-150023