2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Sevabertinib

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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Sevabertinib

Sevabertinib Chemical Structure

CAS No. : 2521285-05-0

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Based on 1 publication(s) in Google Scholar

Sevabertinib Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2].

IC50 & Target

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

Sevabertinib Related Antibodies
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.
Molecular Weight

484.93

Formula

C24H25ClN4O5
CAS No.
Appearance

Solid

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
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 : 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0622 mL 10.3108 mL 20.6215 mL
5 mM 0.4124 mL 2.0622 mL 4.1243 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

SDS (251 KB)

COA (257 KB) HNMR (297 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sevabertinib2521285-05-0BAY 2927088BAY2927088BAY-2927088EGFREpidermal growth factor receptorErbB-1HER1Inhibitorantitumorinhibitorinhibit

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