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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- CAS No.: 2567456-79-3
- Formule: C33H42BrN6O5P
- Masse moléculaire:713.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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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CAS No. 2567456-79-3
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Masse moléculaire 713.60
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HS-10375 Related Classifications
HY-189682 Related Classifications
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