HS-10375
HS-10375 is a selective EGFR tyrosine kinase inhibitor. HS-10375 inhibits EGFR-19del/T790M/C797S-TK and EGFR-L858R/T790M/C797S-TK in an ATP-competitive manner, with IC50 values of 0.09 nM and 0.08 nM, respectively. HS-10375 exhibits higher inhibitory activity against the proliferation of mutant EGFR cells than wild-type EGFR cells, demonstrating selectivity for mutant EGFR and potentially reducing off-target effects. HS-10375 can be used in research related to non-small cell lung cancer.
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- No. CAS: 2567456-79-3
- Fòrmula: C33H42BrN6O5P
- Peso molecular:713.60
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
EGFR-19del/T790M/C797S-TK 和 ，IC50 值分别为 nM 和 。 0.09 nM (IC50) |
EGFR-L858R/T790M/C797S-TK 0.08 nM nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A-431 | IC50 |
138 nM
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Inhibitory activity against A431 cells expressing wild-type EGFR assessed as IC50 by cell-based assay.
Inhibitory activity against A431 cells expressing wild-type EGFR assessed as IC50 by cell-based assay.
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42603542 |
In Vitro
HS-10375 inhibits the proliferation of Ba/F3-EGFR-19del/T790M/C797S-TK and A431 cells with IC50 values of 23 nM and 138 nM, respectively, demonstrating selectivity for mutant EGFR and reducing potential off-target effects[1].
HS-10375 exhibits significant inhibitory activity against mutant EGFR-19del/T790M/C797S-TK and EGFR-L858R/T790M/C797S-TK, with in vitro enzymatic assay IC50 values of 0.09 nM and 0.08 nM, respectively, and an IC50 of 23 nM against wild-type EGFR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 2567456-79-3
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Peso molecular 713.60
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Fòrmula C33H42BrN6O5P
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SMILES
[H][C@]12[C@@]([H])(CN(C(CC3)CCN3C(C=C4OC)=C(C)C=C4NC5=NC=C(Br)C(NC6=CC=C7OCCOC7=C6P(C)(C)=O)=N5)C2)COC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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