Sacibertinib

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Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC₅₀ value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.

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

Sacibertinib Chemical Structure

CAS No. : 1351941-69-9

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•Related Small Molecules:

•Related Proteins:

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TrkA TrkB TrkC Trk

View All EGFR Isoform Specific Products:

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

Biological Activity
Purity & Documentation
References
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Description

Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC₅₀ value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity^[1].

IC₅₀ & Target^[1]

EGFR-TK phosphorylation

110 nM (EC₅₀)

HER2

244 nM (EC₅₀)

In Vitro

Sacibertinib has inhibitory activity against Sk-Br-3, SW620 cells with GI₅₀s of 3.8 nM and 1.78 μM, and against CCRF-CEM/T, Fadu, BxPc-3 and AsPC-1 with IC₅₀s of 5.6 μM, 101 nM, 337 nM and 1 μM, respectively^[1].

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

Molecular Weight

599.08

Formula

C₃₂H₃₁ClN₆O₄

CAS No.

1351941-69-9

SMILES

CN(C)C/C=C/C(NC1=CC(C(NC2=CC(Cl)=C(C=C2)OCC3=CC=CC=N3)=C(C#N)C=N4)=C4C=C1O[C@H]5CCOC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hesheng Zhang, et al. Cyanoquinoline derivatives. CA2802130A1 (Example 138)

[2]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 36, No. 2, 2022.

Sacibertinib Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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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:

Sacibertinib1351941-69-9Trk ReceptorEGFRTropomyosin related kinase receptor Epidermal growth factor receptorErbB-1HER1anticancerantineoplasticInhibitorinhibitorinhibit

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