Lys-PEG3-BA
Lys-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3057939-67-7
- Fòrmula: C38H57ClN9O7P
- Peso molecular:818.34
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas EGFR
More
Actividad biológica
Descripciòn
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
18.56 μM
Compound: Lys-PEG3-BA
|
Inhibition of cell viability in human NCI-H1975 cells incubated for 48 to 72 hrs by CCK8 assay
Inhibition of cell viability in human NCI-H1975 cells incubated for 48 to 72 hrs by CCK8 assay
|
[PMID: 39114932] |
In Vitro
Lys-PEG3-BA (0-20 μM) leads EML4-ALK decertation in H3122 (EML4-ALK) cells and attains a 91% reduction at 10 μM[2].
Lys-PEG3-BA (0-20 μM) specifically triggers the degradation of EGFR in H1975 (EGFR-L858R/T790M) cells, and attains a 52% reduction at 20 μM [2].
Lys-PEG3-BA (48-72 h) efficiently inhibits H3122 (EML4-ALK) and H1975 cell proliferation with an IC50s of 5.30 μM at 48 h and 18.56 μM at 72 h, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:H1975 (EGFR-L858R/T790M) and H3122 (EML4-ALK)
-
Concentration:0, 0.01, 0.1, 1, 10 and 20 μM
-
Incubation Time:48 (for H3122) or 72 h (for H1975)
-
Result:Specifically triggered the degradation of EGFR in H1975 (EGFR-L858R/T790M) cells, without affecting the wild-type EGFR protein level.
Resulted in apparent downregulation of the EML4 ALK protein in H3122 (EML4-ALK) cells at varying doses.
Chemical Information
-
No. CAS 3057939-67-7
-
Peso molecular 818.34
-
Fòrmula C38H57ClN9O7P
-
SMILES
COC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)P(C)(C)=O)=N2)C=CC(N4CCN(CC4)C(CCOCCOCCOCCNC([C@H](CCCCN)N)=O)=O)=C1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
-
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
[1]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
[2]. Zhang J, et al. Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC). J Med Chem. 2024 Aug 22;67(16):13666-13680. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lys-PEG3-BA Related Classifications
HY-180964 Related Classifications
Powered by Bioz