Art. -Nr.: HY-164718

Sevabertinib

(Synonyms: BAY 2927088)

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Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC⁵⁰ <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer.

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Reinheit: 99.90%
CAS. Nr.: 2521285-05-0
Formel: C₂₄H₂₅ClN₄O₅
Molecular Weight:484.93

Speicherung:

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

Sevabertinib Chemical Structure

CAS. Nr.: 2521285-05-0

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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
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC⁵⁰: <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD^[2]

Alle EGFR Isoform-spezifische Produkte anzeigen :

In Vitro

Sevabertinib exhibits an IC⁵⁰ of <0.5 nM against wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD at a physiological ATP concentration of 2 mM, and shows significantly reduced activity against HER4 (IC⁵⁰ = 13.9 nM)^[2].
Sevabertinib potently inhibits the proliferation of isogenic Ba/F3 cells ectopically expressing HER2 exon 20 insertions, activating HER2 point mutations, or putative secondary acquired resistance mutations (T798M, T798I, C805S)^[2].
Sevabertinib potently inhibits the proliferation of two lung cancer cell lines: NCI-H1781 (harboring HER2 exon 20 insertion mutations A775insV and G776C) with an IC⁵⁰ of 19.7 nM, and NCI-H2170 (harboring wild-type ERBB2 amplification) with an IC⁵⁰ of 16.7 nM^[2].

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

In Vivo

Sevabertinib (10-50 mg/kg; p.o.; once daily) inhibits tumor growth and reduces tumor weight in the subcutaneous CTG-2543 PDX mouse model of NSCLC^[2].
Sevabertinib (5-10 mg/kg; p.o.; twice daily for 5 mg/kg; once daily for 10 mg/kg) demonstrates antitumor efficacy in the NCI-H1781 xenograft mouse model, with similar efficacy to Zongertinib (HY-148810)^[2].

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

Animal Model:

Nude mice + subcutaneous CTG-2543 PDX NSCLC model (HER2 A775insYVMA)^[2]
Dosage:

10 mg/kg, 25 mg/kg, 50 mg/kg
Administration:

Oral gavage, once daily (QD)
Result:

Showed T/C ratios of 0.22, 0.12, and 0.06 at doses of 10 mg/kg, 25 mg/kg, and 50 mg/kg, respectively.
Was well-tolerated as no marked body weight loss was observed.

Clinical Trial

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

Chemical Information

CAS. Nr. 2521285-05-0
Appearance Solid
Molecular Weight 484.93
Formel C₂₄H₂₅ClN₄O₅
Color Light yellow to yellow
SMILES

O=C(NCC1)C2=C1NC(C3=CC=NC=C3OC[C@@H]4COCCO4)=C2NC5=C(C(Cl)=CC=C5)OC
Synonyms

BAY 2927088
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (103.11 mM; ultrasonic and warming and heat to 60°C; 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

2.0622 mL

10.3108 mL

20.6215 mL

5 mM

0.4124 mL

2.0622 mL

4.1243 mL

10 mM

0.2062 mL

1.0311 mL

2.0622 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 38, No. 2, 2024.

[2]. Siegel F, et al. Sevabertinib, a Reversible HER2 Inhibitor with Activity in Lung Cancer. Cancer Discov. 2025 Oct 15. [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	2.0622 mL	10.3108 mL	20.6215 mL	51.5538 mL
	5 mM	0.4124 mL	2.0622 mL	4.1243 mL	10.3108 mL
	10 mM	0.2062 mL	1.0311 mL	2.0622 mL	5.1554 mL
	15 mM	0.1375 mL	0.6874 mL	1.3748 mL	3.4369 mL
	20 mM	0.1031 mL	0.5155 mL	1.0311 mL	2.5777 mL
	25 mM	0.0825 mL	0.4124 mL	0.8249 mL	2.0622 mL
	30 mM	0.0687 mL	0.3437 mL	0.6874 mL	1.7185 mL
	40 mM	0.0516 mL	0.2578 mL	0.5155 mL	1.2888 mL
	50 mM	0.0412 mL	0.2062 mL	0.4124 mL	1.0311 mL
	60 mM	0.0344 mL	0.1718 mL	0.3437 mL	0.8592 mL
	80 mM	0.0258 mL	0.1289 mL	0.2578 mL	0.6444 mL
	100 mM	0.0206 mL	0.1031 mL	0.2062 mL	0.5155 mL

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Sevabertinib

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Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sevabertinib Related Classifications

HY-164718 Related Classifications