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.

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Pureté: 98.02%
CAS No.: 2681392-19-6
Formule: C₂₆H₂₄N₁₀O₂
Masse moléculaire:508.53

Stockage:

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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Stock

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Use of MCE Products

Antibody-Drug Conjugates

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

HER2

7 nM (IC₅₀)

ErbB4

EGFR

CDK11B

JAK3

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform PI4K :

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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
Masse moléculaire 508.53
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
- 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)
Instruction de manipulation (2659 KB)

Références

[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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Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform PI4K

Voir tous les produits spécifiques à Isoform CDK

Voir tous les produits spécifiques à Isoform Raf

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

BI-1622 Related Classifications

HY-150023 Related Classifications